| 摘要 |
<p>1,215,379. Piperidyl carbamates. ALDRICH CHEMICAL CO. Inc. 15 Jan., 1968 [16 Jan., 1967], No. 2159/68. Heading C2C. Novel piperidyl carbamates of the formula wherein R 1 is H, C 1-8 alkyl, C 2-8 alkenyl, C 2-8 alkynyl, C 3-7 cycloalkyl, 2-norbornyl, 1-adamantyl or naphthyl group or a group of the formula wherein n is 0 to 5, R<SP>2</SP>, R<SP>3</SP> and R<SP>4</SP> are each the same or different and are H, CP, Br, I, F, CF 3 , C 1-8 alkyl, C 1-8 alkoxy, di-(C 1-8 alkyl) amino, NO 2 , phenyl, phenoxy or benzyl, and Z is C = O or a and the pharmaceutically acceptable nontoxic acid addition salts thereof are prepared either by reacting 1 - [3 - (4 - fluorobenzoyl)propyl]-4- piperidinol, obtained by treating 4-piperidinol with 4-chloro-4<SP>1</SP>-fluorobutyrophenone, or 1,1- ethylenedioxy - 1 - (4 - fluorophenyl) - 4 - (4 - hydroxypiperidino) butane, resulting from the reaction of 4-piperidinol with 4-chloro-1,1- ethylenedioxy - 1 - (4 - fluorophenyl) butane, which is in turn made by refluxing ethyleneglycol, p-toluene sulphonic acid monohydrate and 4-chloro-4<SP>1</SP>-fluorobutyrophenone, with a saturated ethereal solution of phosgene and reacting the thus produced chloroformate hydrochlorides with ammonia or an amine of the formula R 1 NH 2 , or by reacting the above 4- piperidinol derivatives with an isocyanate of the formula R 1 NCO. Therapeutic compositions, having hypertensive and tranquillizing activity in the form of tablets, powders, granules, capsules, suspensions or solutions, contain the above novel piperidine carbamates or pharmaceutically acceptable nontoxic acid addition salts thereof as the active ingredient.</p> |
