| 摘要 |
1,173,833. N,N-Disubstituted amides. MILES LABORATORIES Inc. 25 July, 1967 [1 Aug., 1966], No. 34191/67. Heading C2C. Novel N,N-disubstituted amides of the formula wherein R 1 is C 1-6 alkyl, C 3-6 cycloalkyl, aryl or heterocyclic radical; one of R 2 and R 3 is H, and the other is aryl; and B is an unsubstituted or phenyl- and/or hydroxy - substituted nitrogenous heterocyclic radical connected to the adjacent CH group through a nitrogen atom, and acid addition salts thereof are prepared by acylating the corresponding amines of the formulµ C 6 H 5 CH 2 -NH-CH(R 2 )-CH 2 B or C 6 H 5 CH 2 -NH-CH 2 -CH(R 3 )-B N - (1 - Phenyl - 2 - (4 - phenyl - 1 - piperidyl)- ethyl]-benzylamine is prepared by reducing with LiAlH 4 1 - [α - (benzylamino) phenylacetyl] - 4- phenylpiperidine, obtained by reacting benzylamine with 1 - (α - chlorophenylacetyl)-4-phenylpiperidine, resulting from the treatment of α- chlorophenylacetyl chloride with 4-phenylpiperidine under Shotten-Baumann conditions. N - [1 - Phenyl - 2 - (4 - hydroxy - 4 - -phenyl - 1- piperidyl) ethylbenzylamine is made by reducing with L 1 AlH 4 1 - [α - (benzylamino) phenylacetyl] - 4 - hydroxy - 4 - phenylpiperidine obtained by refluxing 1-(α-chlorophenylacetyl)-4- hydroxy-4-phenylpiperidine with benzylamine. N - [2 - Phenyl - 2 - (4 - phenyl - 1 - piperidyl) ethyl] benzylamine is obtained by reducing with LiAlH 4 N - benzyl - 2 - phenyl - 2 - (4 - phenyl - 1 - piperidyl) acetamide, obtained by refluxing 4- phenylpiperidine with N-benzyl-α-chloro - phenylacetamide, resulting from the reaction of α- chloro-phenylacetyl chloride with benzylamine. Pharmaceutical compositions having analgesic activity comprise as the active ingredients the above novel N,N-disubstituted amides or acid addition salts thereof together with pharmaceutically acceptable carriers or diluents. |
