malvaxman (Hive Bee)
03-14-02 22:38
No 282621
      Easiest way to amphetamine in the kitchen+Fentanyl  Bookmark   

Easiest way to amphetamine in the kitchen... (I think)
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1. Do some nitroethane

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(from:../rhodium/chemistry /nitroalkane.html)


Nitroethane from Sodium Ethyl Sulfate [4]

1.5 mole sodium nitrite (103.5g) is intimately mixed with 1 mole of sodium ethyl sulfate (158g) and 0.0625 moles of K2CO3 (8.6g). The mixture is then heated to 125-130C, at which temperature the nitroethane distills over as soon as it is formed. The heating is discontinued when the distillation flow slackens considerably, and the crude nitroethane is washed with an equal amount of water, dried over CaCl2, and if needed, decolorized with a little activated carbon. The nitromethane is then re-distilled, collecting the fraction between 114-116C. Yield 46% of theory.


Preparation of Sodium Ethyl Sulfate
Method 1 [1]
To prepare the sodium salt of ethyl hydrogen sulfate, a mixture of alcohol and H2SO4 is boiled under reflux, cooled, and an excess of calcium carbonate is added. The ethyl hydrogen sulfate is converted into the soluble calcium ethyl sulfate, whilst the excess of H2SO4 is removed as insoluble calcium sulfate. The aqueous filtrate is then mixed with just sufficient sodium carbonate to give sodium ethyl sulfate, the insoluble calcium carbonate being now filtered off. The solution of sodium ethyl sulfate can be concentrated on the water-bath without appreciable hydrolysis, and the sulfate finally crystallized out.

Place 40ml (32g) of rectified spirit in a 250ml round-bottomed flask, and slowly add. 16ml (30g) of concentrated sulfuric acid, keeping the liquid in the flask well shaken throughout the addition to ensure thorough mixing. Fit a reflux condenser to the flask, and heat the latter on a gauze so that the mixture boils gently for 45 minutes. Then cool the product and pour it into 200ml of cold water contained in a large (8-inch) evaporating-basin or in a shallow earthenware dish. Now add 23g of finely powdered calcium carbonate with stirring to the acid solution. It is essential to add the calcium carbonate as a fine stream of powder, and to stir the latter immediately into the bulk of the solution: for this purpose, it is best to sift the carbonate through a fine sieve directly into the liquid, or alternatively to add it from a spatula, tapping the latter gently over the liquid to ensure steady addition of the finely powdered chalk. If the carbonate is added carelessly several grams at a time, it becomes rapidly covered with insoluble calcium sulfate, which protects it from further reaction: in these circumstances, at least 10 times the theoretical quantity of the carbonate may be required and the evolution of carbon dioxide may continue for several hours. The addition of the calcium carbonate should take about 30 minutes, and the well-stirred mixture should finally be neutral to litmus-paper. Now heat the mixture on a water-bath, using a thermometer as a stirrer, until the temperature reaches 60C, and then filter at the pump through a wide Buchner funnel: at this temperature, filtration should be rapid. Finally wash the residue of calcium sulfate on the filter with a small quantity of hot water, adding the wash-water to the main filtrate. In order to convert the calcium ethyl sulfate to sodium ethyl sulfate, add a concentrated aqueous solution of sodium carbonate cautiously drop by drop to the well-stirred filtrate until a drop of the latter withdrawn on a glass rod is just sufficiently alkaline to turn red litmus-paper blue. Then filter the solution at the pump, and wash the residual calcium carbonate again with a small quantity of water. Evaporate the filtrate on a water-bath until a drop withdrawn on a rod crystallizes on cooling: then allow the solution to stand until almost cold, and finally chill it thoroughly in ice-water. (If the ice-water cooling is omitted, large well-developed colorless crystals of sodium ethyl sulfate will finally separate.) Filter off the crystals at the pump, drain, and dry over calcium chloride in a desiccator. Yield about 12g. To obtain a second (but necessarily less pure) crop of the sulfate, evaporate the filtrate further on the water-bath, and cool as before.
Method 2 [4]

Two moles of absolute ethanol (92 grams) is slowly dripped into a beaker containing one mole of 20% Oleum (H2SO4 containing 20% SO3), adjusting the rate so that the temperature is maintained at 45C. When all the ethanol is added, the solution is neutralized with anhydrous sodium carbonate (Na2CO3), care being taken for the evolution of carbon dioxide. Yield 85% of theory.




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2. DO SOME Phenyl-2-Nitropropene

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Synthesis of Phenyl-2-Nitropropene

(from: ../rhodium/chemistry /phenyl-2-nitropropene.html)
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[ Back to the Chemistry Archive ]
Procedure (By Dreamer)
 
To 55 g (0.5mol) Benzaldehyde in a 500ml Flask were added 40 g (0.5mol) Nitroethane and 10ml Cyclohexylamine. All was refluxed for 6h on a water bath. The result were 2 layers. One orange layer at the bottom with phenyl-2-nitropropene and a clear layer at the top with cyclohexylamine and maybe a little bit (~1ml) of H20. 50ml of H2O were added and then sucked off with a pipette until the phenyl-2-nitro-propene crystallized (it crystallized when it came in touch with air in presence of 15ml H2O). I added 200ml 95% denaturated ethanol to the orange crystals. The color of the now needle-like crystals changed from orange to white-yellow. The crystals were filtered. Yield 65 g, 78% of theory.


(YOU CAN EXCHANGE THE CATALYSATOR CYKLOHEXYLAMINE AGAINST AMMONIUM ACETATE..)

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3.    REDUCE P2NP!

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(from:../rhodium/chemistry /amph.urushibara.txt)

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                          Urushibura Style Amphetamine
                                   by Ritter
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First of all many thanks go to CHEM_GUY for his continuous urging of the Hive
community to try Urushibara Nickel reduction on phenylnitropene. This reduction
turned out to be easier than any so far encountered. This is not based on any of
the excellent references pertaining to Urushibara that have been mentioned on
the hive, only chem_guys postings!

Procedure:

Dissolve 4.0g Nickel Chloride hydrate (light green crystals) in 75 ml 95%
ethanol w/ mag stirring and warming to 50'C. After salt is dissolved remove stir
bar and add 1ml water and 1ml conc. HCl. [1] While solution at 50'C slowly add
5g regular Reynolds wrap torn up into .25 x 1.0in strips in 1g portions with
manual stirring. The aluminum will SLOWLY react with the nickel salt forming the
metal Ni(s) through metathesis as a dark grey chunky powder which settles to the
bottom. A gentle effervescence of hydrogen occurs during reaction. Add aluminum
at a rate that maintains a steady effervescence and keeps temperature roughly in
the 50' range. Note this may take up to two hours!

At the end of Al addition all green color from nickel salt should be discharged.
If any color remains add another gram of aluminum and wait for soln to clear.
Precipitated Nickel powder was added to 100ml 20% NaOH soln and manually stirred
at 60'C for 30 min. Excess NaOH is decanted and nickel is washed with 5 x100ml
aliquots of distilled water to remove excess base. At this point Urishubara
nickel catalyst is prepared and ready for reduction.

Dissolve 5g pure phenylnitropropene in 50ml Ethanol and add to Ni solution [2].
Now slowly add 3ml conc. HCl [3] and 1 gram shredded aluminum w/ manual
stirring. Aluminum will slowly dissolve with a more vigorous effervescence of
hydrogen than the first step. Maintaining good stirring with a glass stirring
rod is essential in beginning. Attempted magnetic stirring will result in
frustration because nickel is ferromagnetic and will stick to stirbar preventing
surface area exposure necessary for reduction. After aluminum is dissolved add
three more milliliters HCl and one more gram Al. Repeat adding acid and Al until
10 grams Al and about 30ml HCl has been added. Aluminum reacts slowly. Expect
addition to take about six hours, longer if temp falls below 50C. Constant
stirring towards end is not necessary, just give mix a good stir occasionally.

After all aluminum is added and mostly decomposed slowly pour in a soln of 30g
NaOH in 100ml H20 with careful stirring. Wear goggles and be careful! Base
neutralization is highly exothermic! In 30 minutes all aluminum sludge will
solvate into bottom aqueous layer and a nice orange alcohol layer reeking of
amine will settle out on top. Nickel is not dissolved by the NaOH so it will
remain floating around between the two layers but this does not present a major
problem. After all, its not poisonous like mercury or anything! Now decant off
the top orange organic layer and distill off alcohol down to a orange stinky
syrup completely different smelling than the P2NP. Dissolve these goodies in
acetone and slowly add sulfuric acid to precipitate the amine sulfate.
Voila!!!!!! about 3 grams light yellow amphetamine sulfate.

[1] Addition of water and acid found to be necessary to initiate rxn between
    NiCl2 and Al.

[2] When nitropropene was added to NiCl2 soln before conversion to Ni powder
    was complete some polymerization occurred greatly reducing yield.
    It seems essential to add P2NP to rxn after Ni is fully precipitated.

[3] Use of Sulfuric acid produced inferior results causing polymerization of
    P2NP to red tar.

Increasing Yield: Use overhead mechanical stirring to keep nickel catalyst
                  better suspended during reduction. Re-extract aqueous NaOH/Al
                  layer w/ toluene and work up in standard manner. Use larger
                  amount of nickel catalyst and more aluminum for H2 generation.

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4. ENJOY!!!!laugh

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    PrimoPyro
(Hive Prodigy)
03-15-02 01:48
No 282711
      Re: Easiest way to amphetamine in the kitchen...  Bookmark   

[pissy_rant]

Why does everybody enjoy reposting what is already documented? What good purpose does this serve?

1.You took this from Rhodium's site, meaning the links and a short description would suffice just dandy.

2.Much of the information on Rhodium's site was taken from Hive discussions! This info is already here! Why repost it?

It is a waste. Links to Rhodium's site with a description of what you are talking about, and post numbers relevant to the topic are all you need. You do not need to repost the entire writeup.


As a side-note, I could not agree more, unless someone has a source of PPA, which is easier to make into amphetamine than this of course. This process is my absolute number one favorite idea for producing amphetamine from scratch.

Amphetamine itself may suck as a stimulant, but there are fucking awesome compounds that can be made from it, that are harder to make when starting from methamphetamine. (although not impossible to do from meth.)

[/pissy_rant]

                                                  PrimoPyro

Vivent Longtemps La Ruche!
 
 
 
 
    malvaxman
(Hive Bee)
03-15-02 20:25
No 283047
      Re: Easiest way to amphetamine in the kitchen...  Bookmark   

There is a purpose in posting it all in one post. I am sure I will make many newbees happy and many bees happy by the fact that newbees will maybee ask fewer stupid question.
All the texts and methods at Rhodiums are difficult to orientate in, specially for newbees and persons without chemisty education.
Many methods which are high yeilding use exotic chemicals and expensive to obtain equipment..
Now when some newbee asks "How do I do amphetamine at home the easiest way", you can link this post..

Now a question for you Primopyro, you write; "Amphetamine itself may suck as a stimulant, but there are fucking awesome compounds that can be made from it".
 Which are those "awesome compounds" you are thinking about, that outclass amphetamine and even meth??? tongue
 
 
 
 
    PrimoPyro
(Hive Prodigy)
03-16-02 01:30
No 283174
      Re: Easiest way to amphetamine in the kitchen...  Bookmark   

They are not stimulants.

Vivent Longtemps La Ruche!
 
 
 
 
    malvaxman
(Hive Bee)
03-16-02 01:42
No 283183
      Re: Easiest way to amphetamine in the kitchen...  Bookmark   

So what compounds which could be made from amphetamine do you enjoy so much???
 
 
 
 
    PrimoPyro
(Hive Prodigy)
03-16-02 04:43
No 283263
      Re: Easiest way to amphetamine in the kitchen...  Bookmark   

I do not enjoy their use, but I do enjoy reading about them. They would be the longer lasting amphetamine based fentanyl analogs. Standard fentanyl is has four major parts to the molecule.

1.The phenyl-alkyl group, that is attached to the N-piperidine structure.

2.The piperidine structure.

3.The anilino structure attached to the 4-piperidine.

4.The propionamide portion of the anilino.

Normally, the first portion is a phenethyl group. There are multiple ways of making the second level precursor: the phenyl-alkyl-piperidone. One way involves chaining the phenylalkyl bromide with piperidone.

Another way uses the phenylalkylamine, and constructs the piperidone ring around it. Phenethylamine would be used in this method as the amine, giving rise to phentanyl. If amphetamine were used, it would give rise to beta-methyl fentanyl I believe it is called by Drone 342, which may not be any more potent, but certainly lasts longer, like all amphetamine versions of phenethylamine drugs.

beta-methyl-3-methylfentanyl would be the strongest opioid I know of, with a dosage of a mere 60mcg for a 220lb (100kg) man, i.v. and it would last longer than the phenethyl version.

Sounds better than meth, no?

                                                     PrimoPyro

Vivent Longtemps La Ruche!
 
 
 
 
    Rhodium
(Chief Bee)
03-16-02 20:39
No 283539
      Re: Easiest way to amphetamine in the kitchen...  Bookmark   

cis-3-methyl-fentanyl has an active dosage of 5-10 mcg (designer drugs directory) - where did you find the activity of cis-3,beta-dimethyl-fentanyl? Logically, it should be even stronger.
 
 
 
 
    obia
(Stranger)
03-16-02 23:59
No 283611
      Re: Easiest way to amphetamine in the kitchen...  Bookmark   

what youre calling beta methyl fentanyl is called alpha methyl fentany AMF in the forensic business. Beta methyl would have the Me next to the phenyl group.
super potent fentanyl homologues could be most interesting if the problems with respiratory depression could be solved the only decent solution i could think of was to use a cut containing small amounts (sub active for a normal dose)but in an od situation enough would be present to prevent death its no good having naloxone/naltrexone unless someone else is there to inject it.
A better solution is to create an euphorient without the other effects, which unfortunately is exactly the opposite to what a pharmaceutical company wants, (how many compounds with the undesirable side effect of creating extreme euphoria but poor analglesia are lurking in pharm company archives?) How about the fentantyl derivative with a methylene bridge across the piperidone portion. the analog with tryptamine replacing phenethylamine could also be entertaining, it would certainly be active.
 
 
 
 
    PrimoPyro
(Hive Prodigy)
03-17-02 02:04
No 283646
      Re: Easiest way to amphetamine in the kitchen...  Bookmark   

malvaxman: Your rebuttal still doesn't explain why retyping it is better than posting links with a description to save space.

Rhodium: I make this assumption to cover my ass. I too think the amphetamine will have higher potency, but I have not read specifically so, so I stay with what I know for certain: amphetamines have longer action than phenethylamines, fentanyls included.

Obia: the stigma is the same the same the same. We're not talking about fentanyl being perfect, but the bottom line is that it is here here and now, not hidden in some future discovery. Its not perfect by any means, but the stigma around it is severely overrated.

Every time a fentanyl discussion arises, the only information to surface is warnings about disaster, etc. Never any real chemistry discussions. All questions are answered with, "Do something simpler first." and all topics on it are altered with negativity about its use.

I personally think this is because people dont have the answers to the questions, so they say what they know. They have heard these stories before, and heard others say its bad its bad its bad, its so dangerous, you'll kill yourself, be careful, you're not ready, try methadone, etc.

Did anyone ask for advice? No. Its a chemistry question. Answer the question. Enter the discussion. Dont have anything to add? Then shut the fuck up.

Obia, this most certainly not directed toward you. You have presented the data initially in the thread, which is good for first time readers, so dont think Im chewing you out, because Im not.

I think its about time for a new, good, fentanyl discussion. I wish Drone were here. He wouldnt listen to the "its dangerous, wha wha wha" bullshit either. All drugs are dangerous. End of story. Fentanyl has special conditions. Work in a glovebox.

Back to a useful discussion: Rhodium, in Post 60132 (Rhodium: "N-phenylethyl-4-piperidones via acrylates", Chemistry Discourse) you say that condensing phenethylamine with two equivalents of methyl methacrylate will give rise to 3-methyl piperidone. I assume this is a typo? Did you mean condense with one equivalent of the methyl methacrylate, and one equivalent of methyl acrylate? Would not two methyl methacrylate additions yield the 3,5-dimethyl-piperidone?

                                                    PrimoPyro

Vivent Longtemps La Ruche!
 
 
 
 
    Chromic
(Hive Addict)
03-17-02 02:30
No 283654
      Re: Easiest way to amphetamine in the kitchen...  Bookmark   

Every time a fentanyl discussion arises, the only information to surface is warnings about disaster, etc. Never any real chemistry discussions. All questions are answered with, "Do something simpler first." and all topics on it are altered with negativity about its use.

Perhaps that's because the people who often engage in such topics don't have enough theoretical framework to get involved with such a conversation or lack the equipment and/or the reagents to perform the appropriate synthesis. However... I'm sure there's a few folk on the Hive who'd love to discuss it with you, unfortunately I'm one of the people who lack both the necessary framework and the necessary reagents, so I'll back out of this topic. frown

P.S. We absolutely need people with a better knowledge of the chemistry than I to participate in this discussion and be able to put together a document such as the one Dal Cason put together for MDxA, ../rhodium/chemistry /mda.dalcason.html I enjoy reading conversations such as the one in this thread, but unfortunately my skills don't allow me to do anything more than follow along with the discussion. (that's why I said I'd back out, as further posts from me would just add clutter that you and I both don't want to read!) smile
 
 
 
 
    PrimoPyro
(Hive Prodigy)
03-17-02 02:34
No 283656
      Re: Easiest way to amphetamine in the kitchen...  Bookmark   

Of course, I understand that caution is adviseable Chromic. Im not some gung-ho idiot looking to make 40 tons of heroin. What I mean is that these warnings have their place, but they appear in places that they are not asked for, such as a synthesis of 4-piperidone for example.

A discussion where I could have learned something suddenly changes to "the dangers of fentanyl" and the thread dies of its own accord. Yes, that really pisses me off. Its like being beaten in the head with "Drugs are bad, mkay?"

Dont back out of a discussion if you have something to say. I certainly dont have any equipment to test these things, but I dont mind talking about them.

                                                   PrimoPyro

Vivent Longtemps La Ruche!
 
 
 
 
    Rhodium
(Chief Bee)
03-17-02 02:45
No 283661
      Re: Easiest way to amphetamine in the kitchen...  Bookmark   

PP: I wondered where you found the dosage information for dimethylfentanyl (you say 60 mcg), as already 3-methylfentanyl is active at 5-10 mcg.

Your correction of my post regarding the michael addition is fully correct, and I have changed my original post to reflect this.
 
 
 
 
    PrimoPyro
(Hive Prodigy)
03-17-02 03:07
No 283670
      Re: Easiest way to amphetamine in the kitchen...  Bookmark   

Rhodium, I am sorry, I had a typo in my post, I meant to say it is at least that potent.

Taken from: ../rhodium/chemistry /carfentanil.html

"For oxalate salt (carfentanyl) ED50 = 0.0006 mg/kg i/v, this mean that for 100-kg body you need only 0.06 mg. FYI, for 3-methylfentanyl (ED50=0.00058 mg/kg i.v.) look up is synthesis in J. Med. Chem. vol 17, No. 10, p. 1047 (1974)."

This is from your carfentanyl synthesis paper on your site. 3-methyl fentanyl is stated to have an effective dose of 0.06mg, which is of course 60mcg.

It is only logical that the even more powerful amphetamine analog would be at least that potent as well, as well as my assumption of longer activity. I had meant to imply that it should be at least as potent as 3-methylfentanyl, the dosage of which I got from your site.

Jesus Christ! I am forgetting that I own certain books! I havent read The Designer Drug Dictionary in a long time! I forgot I even had it! crazy I should have looked there.

Rhodium, I wonder, is the activity of the 3,5-dimethyl-fentanyl less, or what is up with that? It would most certainly be easier to only have to use methyl methacrylate instead of methyl acrylate and methyl methacrylate. The methacrylate would produce the 3,5-dimethyl analog if it worked.

Also, would the methyl interfere with the michael addition? Doesn't the carboxyl end up in the 5 position, or is it the 2/6 position?

                                                    PrimoPyro

Vivent Longtemps La Ruche!
 
 
 
 
    Rhodium
(Chief Bee)
03-17-02 03:45
No 283689
      Re: Easiest way to amphetamine in the kitchen...  Bookmark   

The carboxyl ends up next to the 4-keto group after cyclization, before decarboxylation (that is the 3/5/"ortho" position). If making 3,5-dimethylpiperidones, the carboxy group would be tertiary instead of secondary, right? In that case the method would work very well for that analog in my opinion. I don't have any data on the corresponding fentanyl handy,but it should be in the patent literature.
 
 
 
 
    slappy
(Hive Bee)
03-19-02 08:43
No 284704
      Re: Easiest way to amphetamine in the kitchen+Fentanyl
(Rated as: excellent)
 Bookmark   

3,alpha-Dimethylfentanyl is actually less potent than 3-Methylfentanyl. Again, you can't really combine the features of different Fentanyl's and expect a more powerful analouge. cis-(-)-3-Methylfentanyl is the most powerful 4-monosubstituted anilinopiperidine known. Carfentanil is the most powerful opiate that I am aware of, and both the 3-Methyl and alpha-Methyl homologes of it are less potent than the parent compound. Go figure.

Also, when considering the potency of 3-Methylfentanyl, you have to consider that when you make it, you actually have four isomers, and only one of those posesses the extreme potency.

An added benefit of making 4,4-Disubstituted Fentanyl analoges is that they don't show up on a toxicological screening.
 
 
 
 
    slappy
(Hive Bee)
03-20-02 10:00
No 285252
      'Re: Easiest way to amphetamine in the kitchen+Fen
(Rated as: good read)
 Bookmark   

Actually, there is one compound that I know to be more potent than Carfentanil. It is the Carfentanil skeleton, except with a -CH2CH2COOC(CH3)3 in stead of -CH2CH2Ph on the Piperidinyl Nitrogen. This compound is 1000's of times more powerful than Fentanyl.

You can find it in J. Med. Chem 1991 34(7), 2202-6
 
 
 
 
    Rhodium
(Chief Bee)
03-20-02 22:25
No 285495
      Strongest opiate?  Bookmark   

>1000x Fentanyl, that is right out sick - you'd get respiratory depression just by looking at that compound through a glass window... The N-substituent is tert-Butyl-propionate, right?
 
 
 
 
    PrimoPyro
(Hive Prodigy)
03-21-02 01:57
No 285542
      t-Bu-beta-Alanine  Bookmark   

Could beta alanine { CH2(NH2)CH2COOH } be condensed with t-butanol and a dehydration agent like KHSO4 to its ester like normal carboxylic acids can?

The t-Bu ester of beta-Alanine would be the starting amine for the Michael Addition with methyl acrylate.

And for the other way, the condensation of the bromo compound with piperidone, one would need either 3-bromopropionic acid, or the t-Bu ester thereof.

Could one dehydrate 3-bromopropionic acid and t-butanol with KHSO4 or something similar, to the ester? Will the bromine interfere?

                                                     PrimoPyro

Vivent Longtemps La Ruche!
 
 
 
 
    Rhodium
(Chief Bee)
03-21-02 02:32
No 285559
      Search engines for synthetic pathways  Bookmark   

That sounds like something you look up in the chemical literature instead of thinking it up yourself. I would. I always perform a www.google.com and www.scirus.com search for all the synonyms of small molecules I want to know the synthesis for - it is generally much faster than thinking, and it also verifies any ideas you can think of. Half of the questions I don't know the answer for off the tp of my head can be answered with those search engines.
 
 
 
 
    slappy
(Hive Bee)
03-21-02 06:08
No 285691
      Ahhhh..... [drool]
(Rated as: good read)
 Bookmark   

Let's put it this way, Carfentanil which is over 100x Fentanyl have a ED50 of 520ng/kg, and according to this paper, the N-tert-Butyl Propionate derivative has a ED50 of 28ng/kg. So yes you would probably suffer respitory depression just by looking at it behind glass.wink

Interestingly enough, the U.S.Army holds multiple patents on the synthesis of Carfentanil. It seems as though they had quite an interest in it around the late 70's through the 80's, perhaps for use as a chemical warfare agent?
 
 
 
 
    Rhodium
(Chief Bee)
03-21-02 07:31
No 285741
      Strongest Opiate  Bookmark   

Right... Which means that one gram of that is equivalent to 700-750 kilos of sparkling white pure heroin. Saves quite some space in your stash.

Can't we hijack Eli Lilly's entire workforce to help us make such a simple bioisostere for our beloved LSD molecule?wink
 
 
 
 
    obia
(Stranger)
03-21-02 23:20
No 286043
      strongest opiate  Bookmark   

this beastie would also be legal in many countries provided it was used for er..opening conversations at parties, as a novelty egg timer filling, etc
back to a qualitative aspect I think dipipanone is much nicer than fentanyl. fentanyl is too itchy 
 
 
 
 
    Rhodium
(Chief Bee)
03-23-02 21:43
No 286971
      Opiate  Bookmark   

The opiate mentioned here by slappy is pretty short-acting (80 minutes), but the article sports several even shorter-acting, down to 5 minutes. Interesting.
 
 
 
 
    slappy
(Hive Bee)
03-24-02 18:36
No 287337
      JMC  Bookmark   

Well, that article was about attempts to make short acting fentanyl derivatives.tongue And at 80 minutes, it is not that short-acting. Actually, it is the longest acting of any in that paper including Fentanyl and Carfentanil. The goal of this group, of course, was to find these short acting opiates so that procedures (like minor surgery) could be done on an outpatient basis, very en vouge in todays health care industry. (in America, at least)

I think I got the ED50 those compounds wrong. I don't have the paper at the same location as the computer, so I'm just going from memory.
 
 
 
 
    foxy2
(Distinctive Doe)
03-24-02 19:45
No 287350
      One molecule?  Bookmark   

"Right... Which means that one gram of that is equivalent to 700-750 kilos of sparkling white pure heroin. Saves quite some space in your stash"

Would you get high on ONE molecule of that shit?

Those who give up essential liberties for temporary safety deserve neither liberty nor safety
 
 
 
 
    terbium
(Old P2P Cook)
03-24-02 20:37
No 287356
      Would you get high on ONE molecule of that shit?  Bookmark   

Would you get high on ONE molecule of that shit?
Nah, even a nanogram (10-9 gram) of a substance with a molecular weight of 100 (10+2) contains:

(6X10+23)X(10-9/10+2) =

(6X10+23)X(10-11) = 6X10+12 molecules or six trillion molecules.
 
 
 
 
    Rhodium
(Chief Bee)
03-25-02 00:49
No 287422
      No of brain cells  Bookmark   

And with 100 billion brain cells, there are just 1000 molecules per brain cell available to achieve this effect (not counting the molecules still in the peripheral system), and of course not all neurons sports opioid receptors.
 
 
 
 
    foxy2
(Distinctive Doe)
03-25-02 14:18
No 287618
      Ok ok  Bookmark   

Enough Avagadro already!!!

My thoughts were more along the lines of how in the hell could you ever safely disperse such a substance.  Don't know if i could trust any technique.  At least if I was the one doing it.  Blotters I guess, but I am skeptical of that. 

I wonder what kind of quality controls they put on the fentanyl dispensaries?  Hmmm Six-Sigma just don't seem good enough to me...  Maybee if all your errors were on the low side.blush


How do they accurately make blotters?
Every picture in my mind is of drops, uneven coverage and other shit messing it all up.

Those who give up essential liberties for temporary safety deserve neither liberty nor safety
 
 
 
 
    flipper
(Hive Bee)
03-25-02 14:46
No 287623
      One little question  Bookmark   

Are these the same:

phenethyl-piperidone-4 and 1-(beta-phenethyl)-4-piperidone crazy

You've gotta love me.
 
 
 
 
    PrimoPyro
(Hive Prodigy)
03-25-02 14:53
No 287625
      Yes  Bookmark   

They are, although I believe the first entry is incorrect. I suppose you meant to type phenethyl-4-piperidone, or perhaps phenethyl-piperid-4-one.

But yes, they are the same.

                                                   PrimoPyro

Vivent Longtemps La Ruche!
 
 
 
 
    Rhodium
(Chief Bee)
03-26-02 00:37
No 287814
      blotters  Bookmark   

foxy: from what I have heard, blotters are made by measuring how much ethanol a certain piece of 100-square blotter paper can absorb, then dissolve 100x100g (10mg) LSD in exactly that amount of ethanol, and then spread an even layer of the ethanolic LSD solution on the blotter with an eye-dropper, then allow to dry. The brotherhood of Eternal Love franchised this application procedure to several unemployed people, goes the saying.
 
 
 
 
    foxy2
(Distinctive Doe)
03-26-02 08:03
No 287983
      I still see problems  Bookmark   

Rhodium
Sure that sounds all well and fine for something like LSD, since it ain't going to kiil anybody.

Think about paper chromatography, if you don't apply the liquid nice and evenly then it seems lhighly likely that HOT spots would form. With such potent deadly substances it seems like a gamble.  Maybee using multichannel pipettes to apply it, that would bee best.  Hell YEA, buy one of those automated pipette machines that can load a 96 well plate all at once, then adapt it to loading 96 hit sheets.

Shit one person could cover the opiate supply for the WHOLE WORLD if they had that going.  Imagine THAT!!!

Those who give up essential liberties for temporary safety deserve neither liberty nor safety
 
 
 
 
    Rhodium
(Chief Bee)
03-26-02 08:39
No 287998
      blotters  Bookmark   

That pipetting machine sounds like a good idea.

To avoid "hotspots" being detrimental to the user, do not make the blotter dosage so high that there is any health risk until a whole blotter sheet is ingested at once. As far as I know, carfentanil has such a large therapeutic window that 100x (a whole sheet) the active dose for a non-tolerant subject still is not lethal (don't quote me on this).
 
 
 
 
    terbium
(Old P2P Cook)
03-26-02 20:54
No 288183
      But what does it taste like.  Bookmark   

Shit one person could cover the opiate supply for the WHOLE WORLD if they had that going.  Imagine THAT!!!
My question is which if any of these fentanyls give the desirable heroin like high. Just look in PIHKAL and TIHKAL at the very different highs and effects from variations in the amphetamines, phenethylamines and tryptamines. I would imagine that these synthetic opiods also have a wide spectrum of highs and effects.
 
 
 
 
    slappy
(Hive Bee)
03-27-02 06:22
No 288409
      Fentanyl analo9uges
(Rated as: excellent)
 Bookmark   

Well, we know that Fentanyl gives a rich, heroin like high. And many people think that it is much more euphoric than Heroin even. Also, a-Methylfentanyl which was supposedly very well accepted on the street, along with 3-Methylfentanyl and p-Fluorofentanyl. Many, many Fentanyl analouges have hit the street, more in europe than usa, especially eastern europe. During the 1980's in the Soviet Union, all sorts of different fentanyl's were readily available, and being sold as synthetic herion. After all, the Soviets were very good organic chemists.

Basically, it comes down to receptor binding. The binding effects at the -Opioid receptor are much different than the 5-HT2A receptor. And the effects that the agonists of these receptors manifest are completely different. While these are both G-protein coupled receptors, there is much more of a physiological response from opioid agonists, whereas the Serotonin agonists exhibit a psycological response, which allows much more room for interpetation.
 
 
 
 
    Rhodium
(Chief Bee)
03-27-02 14:20
No 288524
      Opioid receptors  Bookmark   

What would the difference in subjective effects be betwen between hypotetically selective mu, kappa and delta opioid agonists? Which would be the most euphoric, the most addictive, the best pain-killer, the strongest respiratory depressant etc?

What I want to know with this question is what receptor-binding profile would one look for in the pharmacological literature to find potential candidates for the effects one desires?

Are the receptors inter-regulatory, i.e. is it a difference between taking a mixed mu/delta agonist compared to two separate selective mu and delta agonists, provided that the binding is made just as strong by titrating the different dosages?

 
 
 
 
    flipper
(Hive Bee)
03-27-02 19:04
No 288582
      question  Bookmark   

When I make a list of of all the chemicals used to synthesize carfetanil and fentanil ( maybe I didn't spelled it ride but whatever) It's a huge list. Can I shorten this list by say uing only MeOH or EtOH as solvent or use only one kind of dryingagent, without affecting the yield.

You've gotta love me.
 
 
 
 
    slappy
(Hive Bee)
03-27-02 19:11
No 288584
      Receptor profiles
(Rated as: excellent)
 Bookmark   

The kappa and delta receptors play no real part in the effects you mentioned (euphoria, addictiveness, pain-killing, respiratory depression). Those are all effects are generally attributed to the -Opioid receptor. At the cellular level, they all activate G-proteins (35S-GTP gamma-S binding), activate inwardly rectifying K+ channels, inhibit calcium Ca2+ currents, and inhibit adenylyl cyclase, but the mu obviously posses many other properties that have yet to be fully extrapolated. We stil don't really understand any of the receptors. It is only in the last few years that they have been able to solve the exact structure of the various receptors by x-ray crystallography and protein NMR. Having the full structural conformation of the receptors allows us to better understand ligand docking, but we're still clueless about how the subjective effects are actually elicited. Apperently, when the ligand finds it's way into the binding pocket, and arranges itself into it's binding conformation by coordinating with the active sites on the amino acid residues in protein pocket, and the protein actually changes shape, rearranges to it's "agonized" conformation until the ligand detaches. This, of course is what elicits the subjective effects.

For our purposes, there are a select few receptors that we are looking to target, namely the -Opioid, 5-HT2A, CB1 Cannabinoid, Etc. This is, of course, not meant to imply that the other receptor subtypes are without merit, just that for what we are looking for (= fun compounds), they're just not the place to be.

I just came across an interesting compound. N-(4-Bromobenzyl)-5-Methoxytryptamine. Apperently it is a very potent and selective ligand for the 5-HT2A receptors (Ki= 0.1nM) It was reported by Glennon et al: "Influence of amine substituents on 5-HT2A versus 5-HT2C binding of phenylalkyl- and indolylalklamines." J. Med. Chem. 1994 37 1929.

This could very easily be made from 5-Methoxytryptamine (which could be made from melatonin) by reacting with 4-Bromobenzylchloride in CH2Cl2 catalysed by DMAP or Hnig's Base (DIPEA).
 
 
 
 
    flipper
(Hive Bee)
03-27-02 23:09
No 288678
      asking for the answer  Bookmark   



flipper
Hive Bee)
03-27-02 19:04
Post 288582 (flipper: "question", Methods Discourse)      

When I make a list of of all the chemicals used to synthesize carfetanil and fentanil ( maybe I didn't spelled it ride but whatever) It's a huge list. Can I shorten this list by say uing only MeOH or EtOH as solvent or use only one kind of dryingagent, without affecting the yield.




Well?????? cool


You've gotta love me.
 
 
 
 
    slappy
(Hive Bee)
03-28-02 00:03
No 288698
      Hmmm... no.  Bookmark   

You are definatly not in a position to be making Carfentanil. You don't yet have the experience to be handling such incredibly toxic compounds. I know you want to make Fentanyl and LSD, and I think nothing wrong with that, but you are going to need some more experience before approaching these kind of synthesis. Otherwise you'll end up killing yourself and (god forbid) a host of users downstream of you.

To answer your question, no. There are times for alcohol, and there are times for aprotic solvents.
 
 
 
 
    Rhodium
(Chief Bee)
03-28-02 00:56
No 288738
      Opioid Receptors  Bookmark   

But Slappy, there must be some relatively selective kappa and delta opioid agonists, right? If almost all the classic effects are mediated via the -receptor, what does relatively selective kappa/delta agonists feel like? Or are there none that selective found yet?
 
 
 
 
    Ritter
(Master Whacker)
03-28-02 02:18
No 288766
      Delta and Kappa agonists
(Rated as: excellent)
 Bookmark   

Rhodium,

Check this paper out:  J. Med. Chem. 2002, 45, 537-540

This paper is excellent, has info on some really cool oxycodone congeners with VERY high kappa and delta receptor affinity and little mu agonistic activity.  There is also an analogue with extremely high Mu affinity, it is an adduct of B-nitrostyrene(isn't that cool!)  and N-Benzylimino-oxyxocone.  It's a simple procedure with a decent yield.

I can post the .PDF on request.
 
 
 
 
    slappy
(Hive Bee)
03-28-02 02:28
No 288771
      delta, kappa agonists
(Rated as: excellent)
 Bookmark   

There are a whole slew of agonists selective fo the delta and kappa opioid receptors, just look in your Sigma or Tocris catalog or the like. There are many ligands with >nM affinity for a certain receptor subtype even. Most of the opioid ligands are peptides, like our endogenous -agonists, the Endomorphins, or Deltorphin for the kappa. Some examples of specific non-peptide agonists are: SB 205607, SNC 80, SNC 121 (delta) and BRL-52537, ICI 199,441, N-Methyl-N-[(1S)-1-Phenyl-2-(1-pyrrolidinyl)ethyl]phenylacetamide HCl, (-)-U-50488, U-54494A (kappa). All three receptors also have a variety of selective antagonists.

As you can tell, these are all experimental probes for neuroscience research. A delta or kappa agonist would never be commercialized, at least not as an analgesic, because they just don't posses those properties. Many opiates on the market posses delta and kappa agonizing properties, but that is just peripheral to the action.

There is also one more opioid receptor, the Orphan Opioid Receptor ORL1 (Opioid Receptor-Like1) that has a high degree of homology with the mu, delta, and kappa receptors, but a distinctly different pharmacological profile. i.e., it looks and acts like the other opioid receptors, but doesn't produce any effetcs that would normally be attributed to that family other than adenylyl cyclase inhibition.

I have ingested a selective kappa agonist before, and the only effects it seemed to produce was a slight headache and nausea.
 
 
 
 
    flipper
(Hive Bee)
03-28-02 07:34
No 288873
      You can tell me  Bookmark   

You can tell me.


crazyredhead
03-25-02 23:01
Post 287764 (crazyredhead: "Massive Renovation In Newbee Forum", Newbee Forum)

Massive Renovation In Newbee Forum  

Third rule -- No discussion of ongoing or planned criminal activity. This board is a place for learning "theoretical" synthesis. A simple guideline for appropriate posts is to always keep them impersonal and timeless. For example  "swim dreamt about another life where he........."




Pleasure me. smile smile smile smile


You've gotta love me.
 
 
 
 
    flipper
(Hive Bee)
03-28-02 18:35
No 289076
      ooooh  Bookmark   


slappy
(Hive Bee)
03-28-02 00:03
Post 288698 (slappy: "Hmmm... no.", Methods Discourse)
       

To answer your question, no. There are times for alcohol, and there are times for aprotic solvents.




Damn,I really need glasses. You had answered my question and I missed it.
Thank you Slappy. I think I was stil sleepy because I had just wake-up when I read your post. Sorry, my mistake. crazy crazy Crazy me crazy crazy    
 


You've gotta love me.
 
 
 
 
    Cyrax
(Hive Bee)
09-10-02 16:19
No 354900
      Ultrashort- and Ultrapotent Fentanyl Analogs
(Rated as: excellent)
 Bookmark   

Slappy said: Well, we know that Fentanyl gives a rich, heroin like high. And many people think that it is much more euphoric than Heroin even.

Well, I disagree.  Morphine is more euphoric than fentanyl.
What few people know is that fentanyl is actually less addicting.  The withdraw is not as tough as with morphine / heroin, probably because the dose is so small (and because it is not as good).  The only fentanyl that could compete with heroine is probably 3-methyl fentanyl.  The narcotic effects have about the same duration as heroin (4 hours).  The long duration is due to the pseudo irreversible binding to the receptor.
Furthermore, a positive thing however is that fentanyl does not induce such a histamine release as morphine.

Slappy's article (cfr supra Post 285252 (slappy: "'Re: Easiest way to amphetamine in the kitchen+Fen", Methods Discourse)) is available here:

Design, Synthesis, and Pharmacological Evaluation of Ultrashort- to Long-Acting Opioid Analgetics
Paul L. Feldman, Michael K. James, Marcus F. Brackeen, Joanne M. Bilotta, Suzanne V. Schuster, Avis P. Lahey,
Michael W. Lutz, M. Ross Johnson, and H. Jeff Leighton

J. Med. Chem. 34(7), 2202-6 (1991) (../rhodium/pdf /ultrashort.ultrapotent.fentanyl.pdf)

Abstract
In an effort to discover a potent ultrashort-acting p opioid analgetic that is capable of metabolizing to an inactive species independent of hepatic function, several classes of Canilidopiperidine analgetics were synthesized and evaluated. One series of compounds displayed potent p opioid agonist activity with a high degree of analgesic efficacy and an ultrashort to long duration of action. These analgetics, 4-(methoxycarbonyl)-4-[(l-oxopropyl)phenylamino]-lpiperidinepropanoic acid alkyl esters, were evaluated in vitro in the guinea pig ileum for p opioid activity, in vivo in the rat tail withdrawal assay for analgesic efficacy and duration of action, and in vitro in human whole blood for their ability to be metabolized in blood. Compounds in this series were all shown to be potent p agonists in vitro, but depending upon the alkyl ester substitution the potency and duration of action in vivo varied substantially. The discrepancies between the in vitro and in vivo activities and variations in duration of action are probably due to different rates of ester hydrolysis by blood esterases. The SAR with respect to analgesic activity and duration of action as a function of the various esters synthesized is discussed. It was also demonstrated that the duration of action for the ultrashort-acting analgetic, 8, does not change upon prolonged infusion or administration of multiple bolus injections.
 
 
 
 
    Antoncho
(Official Hive Translator)
09-10-02 17:50
No 354912
      Slappy! Ritter!  Bookmark   

Despite my disinterest in opiates as recreationals, this thread has been a VERY interesting read.


Ritter, please, post that PDF!



Yours,


Antoncho
 
 
 
 
    Rhodium
(Chief Bee)
09-10-02 22:18
No 354977
      4-arylpyrrolomorphinans.pdf
(Rated as: excellent)
 Bookmark   

Ritter's find from J. Med. Chem. 2002, 45, 537-540 is now available here:

4'-Arylpyrrolomorphinans: Effect of a Pyrrolo-N-benzyl Substituent in Enhancing sigma-Opioid Antagonist Activity

../rhodium/pdf /4-arylpyrrolomorphinans.pdf

The development of selective antagonists for mu, sigma, and kappa opioid receptors has allowed both the role of these receptors to be defined and the selectivity of agonists to be determined. The functions in which  receptors are implicated are quite varied. sigma Agonists were first of interest as offering analgesia without the problems associated with the traditional mu agonist analgesics, e.g., morphine. But sigma agonists also have antidiarrheal effects without affecting gastric mobility and are immunostimulants and stimulants of respiration. sigma Antagonists are immunosuppressants and prevent the development of tolerance and dependence with mu agonists so that opioids with mixed mu agonist, sigma antagonist profiles have beeen recognized as having potential as analgesics for the relief of severe pain.
 
 
 
 
    Cyrax
(Hive Bee)
09-11-02 12:41
No 355274
      What few people know is that fentanyl is actually ...  Bookmark   

What few people know is that fentanyl is actually less addicting.  The withdraw is not as tough as with morphine / heroin, probably because the dose is so small (and because it is not as good).

This also in contradiction with what has been written in post Post 347651 (raffike: "Actually fentanyl and it's analogues cause harder ...", General Discourse):
Actually fentanyl and it's analogues cause harder addiction than H cuz it's said to be better than ol' brown H


I just wanted to straighten this out.  Again, just because a compound is more powerfull (lower ED50) it doesn't necessarily imply that it is better and / or more addictive.

Furthermore, p-fluoro-fentanyl seems to be more morphine like than fentanyl.
The order of receptor affinity of morphine is mu > delta > kappa, whereas in fentanyl and sufentanil the order is somewhat reversed (mu > kappa > delta).  p-fluoro-fentanyl has the same order of binding affinity to the receptors as morphine, with the only difference that it binds
49 x stronger to the mu receptor,
7 x stronger to the delta receptor,
and 5 x stronger to the kappa receptor
than morphine.

For comparison, fentanyl binds
7 x stronger to the mu receptor,
0.9 x stronger to the delta receptor,
and 2.8 x stronger to the kappa receptor
than morphine.

And sufentanil binds
24 x stronger to the mu receptor,
3.7 x stronger to the delta receptor,
and 14 x stronger to the kappa receptor
than morphine.

So, p-fluoro-fentanyl is stronger than sufentanil.
And o-fluoro-fentanyl is even stronger than the para isomer.  That compound would blow the crap out of you, even by looking at it ...

Who said p-fluoro-fentanyl is weaker than fentanyl ... hmm let me see.



Maintenant, je suis cass crazycrazycrazysmiletonguetonguewink  ggrrrrrr ...