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All 2 posts   Subject: Substituted N-Phenylpropanamides   Please login to post   Down

 
    pHarmacist
(pHantasticant)
06-05-03 17:21
No 438010
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      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. (https://www.rhodium.ws/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.

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

Accept No Imitations, There Can Only Bee One; www.the-hive.ws
 
 
 
 
    murmur
(HyperLab Bee)
06-09-03 08:57
No 438798
      Janssen
(Rated as: good read)
    

There are some related patents: Patent US3907811 and Patent US3907813
 
 

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