Author Topic: Analgesic Patent  (Read 2341 times)

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Bwiti

  • Guest
Analgesic Patent
« on: August 15, 2002, 01:36:00 PM »
While farting around at

http://gb.espacenet.com/

, I found a patent that I think is interesting:

GB801577
Lower alkyl 4-phenyl-1-(hydrocarbyl) piperidine-4-carboxylates and the preparation thereof


http://l2.espacenet.com/espacenet/viewer?PN=GB801577&CY=gb&LG=en&DB=EPD



Love my country, fear my government.

Cyrax

  • Guest
Those precious little analogs
« Reply #1 on: August 15, 2002, 02:36:00 PM »
Interesting, hmm ..., it most definitely is.

This ethyl 4-phenyl-1-(3-phenylpropyl)-piperidine-4-carboxylate seems to be a hybrid between pethidine (the phenyl & the ethyl carboxylate on the 4 position in the piperidine ring) and phenoperidine (the 3-phenylpropyl group on the N of the piperidine ring - although it is a 3-phenyl-3-hyrdroxy-propyl group in the case of phenoperidine).  Phenoperidine, which is a kind of pethidine reversed esther, is 25 - 50 times as powerfull as morphine.  Hence, I think that the reversed esther of 4-phenyl-1-(3-phenylpropyl)-piperidine-4-carboxylate would be more powerfull than the 14 x pethidine.  It would be the phenoperidine minus the 3-hydroxy.  Reversed esters are always more potent than the corresponding pethidine analog.

The only problem with this patent would be the synthesis of the ethyl 4-phenylpiperidine-4-carboxylate hydrochloride precursor.  This is not like a easy thing to do  :( .

For mor information about pethidine & analogs see:

http://www.undcp.org/bulletin/bulletin_1957-01-01_4_page006.html#s12