06-05-03 10:21
No 438010
      Substituted N-Phenylpropanamides
(Rated as: excellent)

Synthetic analgesics. Synthesis and pharmacology of the diastereoisomers of N-[3-methyl-1-(2-phenylethyl)-4-piperidyl]-N-phenylpropanamide and N-[3-methyl-1-(1-methyl-2-phenylethyl)-4-piperidyl]-N-phenylpropanamide
Willem F. M. Van Bever, Carlos J. E. Niemegeers, Paul A. J. Janssen;
J. Med. Chem.; 1974; 17(10); 1047-1051. (../rhodium/pdf /fentanyl/3-methylfentanyl.diastereomers.pdf)

Abstract: The synthesis of the respective diastereoisomers and enantiomers of N-[3-methyl-1-(2-phenylethyl)-4-piperidylj-N-phenylpropanamide and N-[3-methyl-l-(l-methyl-2-phenylethyl)-4-piperidyl]-N-phenylpropanamide is reported. Analgesic activity is evaluated in the tail withdrawal test in rats. cis-(+)-N-[3-Methyl-l-(2-phenylethyl)-4-piper-idyll-N-phenylpropanamide (23) is found to be an extremely potent analgesic, up to 6684 times morphine. Compound 23 has a fast onset of action, a shorter duration of action than morphine, and an unusually high safety margin.

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Janssen is the ultimate authority when it comes to synthing far-out potent opioids...

Accept No Imitations, There Can Only Bee One;
(HyperLab Bee)
06-09-03 01:57
No 438798
(Rated as: good read)

There are some related patents: Patent US3907811 and Patent US3907813