dormouse (Member)
04-23-00 02:32
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      synthesis of bupropion,zybian,wellbutrin,... -timeless  Bookmark   


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Author  Topic:   synthesis of bupropion,zybian,wellbutrin,... 
timeless
Member   posted 04-08-99 04:32 AM          
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Synthesis of Bupropion HCl
from ibm us patent server (US patent 4347178);


Lets start with 3-chloropropiophenone which you can buy from aldrich(250gr
200DM) or if someone has a nice idea how to synthisize it, plz tell;

0.16 mol of 3-chloropropiophenone was dissolved in 40-50ml of mathanol and
2 drops of conc HCl were added. Add over a period of 10-15 minutes 0.16
mol of Bromine; Then all was heated over a steam bath allowing much of the
solvent to evaporate; all was washed with cold water and then recrystallized
severall times from hexane;
Yield 90% with methyl 2-[2chloro-4-(2-bromopropionyl)phenoxy]acetat


0.1mol of the above cristalls were dissolved in 20ml acetonitril and 0.44mol
of t-butylamin was added. All was left overnight at 40 and in the morning the
mixture was heated on a steam bath, allowing solvent and excess amine to
evaporate(dryness).The residue was treated with cold water and NaOH to ph 11
and extracted quickly with ether. The etheral extracts were dried over
anhydrous sodium sulfat and then the ether and any traces of t-butylamin were
removed by evaporation. Then the residue was dissolved again in ether and the
hydrochloric salt precipitated after the addition of alcoholic HCl This was
then recrystallized from methanol - ethyl acetat - ether. You will get
Bupropion HCl.

Yield 65% with 2-[2-chloro-4-(2-t-butylaminopropionyl]phenoxyacetal hydrochloride. It should
obviously work with bupropion too. And it should be possible to scale all up.

Bupropion ( Amfebutamone, Wellbutrin )

Bupropion ( Wellbutrin ) has a stimulant type of effect and is used primarily for the treatment of major depression. Bupropion ( Wellbutrin ) can also be used to treat ADHD, Bipolar depression, treat chronic fatigue syndrome, in reducing cocaine craving, to help kick smoking, and to reduce lower back pain.
Bupropion ( Wellbutrin ) was released for use in the United States of America in 1989. About 28% of persons taking this drug will loss five or more pounds and about 0.04% will experience seizures.

CLASS: Monocyclic Aminoketone.
Generic name: Bupropion Hydrochloride.
Type: Antidepressant.

Strengths:

Dosages:
Actual dosage must be determined by the physician.

Prolonged usage: Check kidney / liver function. Check blood levels of serum bupropion.

Oral:
Start: 100 mg in the morning and then 100 mg in the evening, 200 mg total daily.
Increases: After three days, 100 mg morning, 100 mg noon, and 100 mg evening ( 6 hours apart and continued for 3 or 4 weeks. ) May be increased slowly up to 450 mg daily. Increases should not be greater than 100 mg daily over a 3 day period.
Maximum: 450 mg in 24 hours.

Approximately four in every thousand will have seizures.
Higher doses increase risk of seizures.

Normal dosage:
If under 18 years of age, DO NOT USE!
18 to 60 years of age, 200 mg in two doses.
Over 60 years of age, Lower dosage increased cautiously.

Problems with:
Liver Function: Lower dosage, as needed with careful monitoring.
Kidney Function: Must lower dosage, as needed.

Test:

Before taking: None.
While taking: None.

Take With: Empty stomach and a full glass of water. Can be taken with food to lessen stomach irritation.

Full Benefits In: In three or four weeks.

Missed Dose(s): If within one hour take, if over an hour skip and then continue on your normal schedule.
Never Take a Double Dose!

If Stop Taking: Do not stop without consulting your physician and never abruptly.

Overdose symptoms include: Heart failure, hallucinations, loss of consciousness, rapid heartbeat, or seizures.

Warnings
Important: Do not take this drug if you are taking any type of monoamine oxidase inhibitor ( MAO ) or have taken one within the past two weeks.
Do not take this drug if you have any type of seizure disorder.
Do not take this drug if you have a history of anorexia or bulimia.
Do not drink alcohol while taking this drug.
Do not take this drug if you are pregnant. Try some non-drug alternatives.
Do not take this drug if planing to become pregnant. Do not take if you are breast-feeding.
Do not give this drug to any one under eighteen. If over sixty only use drug in small doses and with close monitoring of its side effects.
The habit-forming potential is none.
Do not use if: You had negative reactions to this drug in the pass. If you have a history of epilepsy, bulimia, or anorexia.

Inform your Doctor:
If you have had a negative reactions to this drug in the past.
If you have epilepsy.
If you have heart, liver, or kidney disease.
If you have a history of alcoholism or drug abuse.
If you are taking any other prescription or non-prescription drugs.
Including any anti-psychotic or anti-depressant type drug:
Clozaril, Dilantan, Haldol, Larodopa, Lithium, Loxapine,
Maprotiline, Molindone, Phenobarbital, Phenothiazines,
Prozac, Tagamet, Thioxanthenes, Trazodone, or Tegretol.
If you will be under anesthesia or have any surgery in the next few months.
If you will be undergoing any medical tests.


Bupropion ( Symptoms or Effects )
Common: Agitation, change in appetite, constipation, diarrhea, dizziness, dry mouth, headache, increased perspiration, insomnia, nausea, or vomiting.
Rare: Acne, blurred vision, chest pain, chills, coordination problems, confusion, decrease in white blood cell count, fainting, fever, gum irritation, hair color changes, hair loss, hallucinations, hives, indigestion, itching, liver toxicity, loss of movement, nightmares, racing heartbeat / palpitations, seizure, skin rash, sexual problems, suicidal thoughts, tinnitus ( ringing in the ears ), excessive thirst, toothaches, tremors, urinary problems, or weight gain / loss.
See physician always: Acne, blurred vision, chest pain, chills, coordination problems, confusion, decrease in white blood cell count, fever, gum irritation, hair color changes, hair loss, hallucinations, hives, indigestion, itching, liver toxicity, loss of movement, racing heartbeat / palpitations, seizure, skin rash, sexual problems, suicidal thoughts, tinnitus ( ringing in the ears ), excessive thirst, toothaches, tremors, urinary problems, vomiting, or weight gain / loss.
See physician if severe: Agitation, change in appetite, constipation, diarrhea, dizziness, dry mouth, headache, increased perspiration, insomnia, nightmares, or nausea.
See physician NOW: Skin rash.
Stop taking and see physician NOW: Fainting or Seizures.

by Timeless


 
Barracuda1965
Member   posted 04-09-99 01:20 PM          
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Question.
What is the recreational value of Wellbutrin?
It was once prescribed to me and all I seem to recall it doing was increase my perspiration.

------------------
'Cuda65


 
Beagle
Member   posted 04-11-99 12:10 AM          
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Recreational value nonexistant.
Value as an effective antidepressant or for treatment of adult ADD high. Possibility that it may decrease craving for stimulants: maybe.

Regarding synthesis of alpha-Br-3-Cl-propiophenone, anyone know the reason that conc HCl was used?

Regarding synthesis of this compound:
A) 3-Cl-propiophenone from chlorobenzene and propionyl chloride/AlCl3 w/ careful control of conditions?
B) why bother. Easily obtainable from physician.


dtcc
Member   posted 04-16-99 12:50 PM          
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My 300mg daily dosage must then explain my decreased appetite for speed as well as a smoke free 2 weeks! Yes, but other than that, not a recreational drug at all. If you read the paper on lycaeum discussing the negative effects of disassociatives, it claims in there to aviod Bupropion at all costs when using disassociatives. So stay off the K if you enjoy your current mental capacity.
 
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