| 摘要 |
1,214,077. Oxime carbamoyl esters. USV PHARMACEUTICAL CORP. 27 Sept., 1968 [2 Nov., 1967 (2); 20 March, 1968; 5 Aug., 1968], No. 46134/68. Heading C2C. Novel oxime carbamoyl esters of the formula wherein R 1 is C 1-5 alkyl, C 2-5 alkyl, cycloalkyl, aryl, substituted aryl, heterocyclic or substituted heterocyclic; R 2 is H, C 1-5 alkyl, C 2-5 alkenyl, or phenyl-C 1-5 alkyl; R 3 is C 1-5 alkyl, C 2-5 alkenyl, cycloalkyl, phenyl, substituted phenyl, heterocyclic or substituted heterocyclic; Y is C 1-5 alkylene, and X is di-(C 1-5 alkyl) amino,benzylethylamino,di-(C 2-5 alkenyl) amino, benzylethyl amino, di-(C 2-5 alkenyl) amino, di- (cycloalkyl) amino, N-(C 2-5 alkenyl)-N-(C 1-5 alkyl) amino, pyrrolidino, piperidino, morpholino, thio morpholino, homopiperidino, piperazino or N-methylpiperazino and pharmaceutically acceptable acid addition salts thereof are prepared by reacting ketones of the formula with hydroxylamine derivatives of the formula wherein Z is H or CON(R 2 )R 3 , and, when Z in the resulting products is H, reacting them with either isocyanates of the formula or carbamoyl halides or esters of the formula and, if desired, converting compounds of Formula I wherein R 2 is H to those where R 2 is C 1-5 alkyl or phenyl-C 1-5 alkyl by alkylation. 4 Dimethylaminobutyrophenone oxime N,N- dimethylaminovalerophenone oxime and 3-(N,N- dimethylamnino) - 3<SP>1</SP>- chloropropiophenone oxime are prepared by reacting the appropriate aminoketones with hydroxylamine hydrochloride. 4 - Dimethylaminobutyrophenone oxime hydrochloride is made by treating the free base with ethanolic hydrogen chloride. Pharmaceutical compositions having analgesic activity and suitable for oral, parenteral, rectal or topical administration, contain the above novel compounds or pharmaceutically acceptable acid addition salts thereof and suitable carriers or diluents. In addition to the above mentioned analgesic activity some of the compounds also possess anticonvulsant, hypotensive and topical anaesthetic activities. |
