| 摘要 |
1493222 Cycloalkanone-oxime ethers EGYT GYOGYSZERVEGYESZETI GYAR 27 Jan 1976 03176/76 Heading C2C Novel compounds I and acid addition and quarternary ammonium salts thereof in which R is phenyl optionally substituted by a halogen atom or by one or more, C 1-4 alkoxy OH, NO 2 or di C 1-3 alkylamine groups, R 1 and R 2 are H or together represent a bond, A is C 2-4 alkylene and B is NR<SP>3</SP>R<SP>4</SP> (where R<SP>3</SP> and R<SP>4</SP> are H or both C 1-4 alkyl or R<SP>3</SP> and R<SP>4</SP> together represent C 4-7 alkylene optionally interrupted by O, NH, N-C 1-3 alkyl or N-benzyl) and n is 3 to 10; are prepared by (1) reacting an oxime B-AONH 2 with (a) the corresponding ketone or thioketone or (b) a compound IV or (2) reacting the corresponding unsubstituted oxime with a compound B-A-Hal or with Hal-CH 2 -A<SP>1</SP>-Hal followed by aminating with NHR 3 R 4 (where Hal and Hal<SP>1</SP> are halogen and A<SP>1</SP> is C 1-3 alkylene); and, if desired, forming a salt thereof or treating a salt formed to produce the free base. 2-Benzylidene-cyclohexanethione is prepared by reacting cyclohexanethione with benzaldehyde. Compounds I have local analgesic, spasmolytic, nicotine-lethality inhibiting, tetrabenazine antagonistic and tetracor-spasm inhibiting properties and form with a carrier diluent and/or auxiliary agent a pharmaceutical composition which may be administered orally or parenterally. |
