| 摘要 |
<p>1,178,034. N - Hydroxycyclohexyl - benzylamine derivatives. KARL THOMAE G.m.b.H. 3 May, 1967 [10 May, 1966; 29 June, 1966], No. 20661/67. Heading C2C. Novel N - hydroxycyclohexyl - benzylamine derivatives of the general formula wherein Hal is a chlorine or bromine atom, R<SP>1</SP> is a hydrogen, chlorine or bromine atom and R<SP>2</SP> is a hydrogen atom or methyl group, and acid addition salts thereof are prepared (a) when R<SP>1</SP> is chlorine or bromine, by nuclear chlorination or bromination of an N-hydroxycyclohexylaminobenzylamine of the formula (b) by deacylation of an acyl derivative of the formula wherein R<SP>3</SP> is a protecting aliphatic or aromatic acyl group and R<SP>4</SP> is a hydrogen atom or a proteeting aliphatic or aromatic acyl group; (c) by reduction of a nitro compound of the formula or (d) by reduction of an N-hydroxycyclohexylbenzamide derivative of the formula with a complex metal hydride; followed by optional salt formation or conversion of a resulting salt to the free base form. Pharmaceutical compositions having antipyretic, secretolytic and antitussive activity comprise, as active ingredient, at least one N- hydroxycyclohexyl-benzylamine derivative of the first general formula above or a non-toxic acid addition salt thereof, together with a pharmaceutical carrier or excipient.</p> |
