Author Topic: Substituted N-Phenylpropanamides  (Read 7175 times)

0 Members and 1 Guest are viewing this topic.


  • Guest
Substituted N-Phenylpropanamides
« on: June 05, 2003, 10:21:00 AM »
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;



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.

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


  • Guest
« Reply #1 on: June 09, 2003, 01:57:00 AM »
There are some related patents:

Patent US3907811


Patent US3907813