process for the production of new 1 - (4 - oxo - 4 - (four countries) - butyl) - piperidine

摘要

Novel 1 - [4 - oxo - 4 - (4 - fluorophenyl) - butyl]-piperidine of the general formula FORM:1085429/C2/1 wherein R1 represents a hydrogen, fluorine, chlorine or bromine atom or a methyl, hydroxy or methoxy group; R2 represents an alkyl group having from 1 to 8 carbon atoms or a cycloalkyl or phenyl group; and R3 represents a hydrogen atom or an a - or b -methyl group; and acid addition salts thereof are prepared by condensation of a secondary piperidine derivative and a 4 - X - 1 - (4 - fluorophenyl) - butanone - 1 of the corresponding formulae FORM:1085429/C2/2 FORM:1085429/C2/3 wherein X represents a group which can be eliminated with the hydrogen atom attached to the nitrogen atom of the piperidine ring, followed by optional conversion to an acid addition salt of the product. Pharmaceutical compositions comprising as active ingredient at least one compound of the first general formula above or non-toxic acid addition salt thereof in conjunction with a pharmaceutical carrier or excipient have valuable analgesic and neuroleptic activities. The compositions may be in a form suitable for oral, rectal or parenteral administration.