Bwiti
(PVC-Analog Taste-Tester)
08-15-02 13:36
No 345641
       Analgesic Patent  Bookmark   

  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
(Hive Bee)
08-15-02 14:36
No 345650
       Those precious little analogs  Bookmark   

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 frown.

For mor information about pethidine & analogs see: http://www.undcp.org/bulletin/bulletin_1957-01-01_4_page006.html#s12