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EP0812827A1 Piperidine derivative as intermediates for the preparation of paroxetine and process for their preparation 失效
哌啶衍生物作为中间体用于帕罗西汀的制备和它们的制备方法

Piperidine derivative as intermediates for the preparation of paroxetine and process for their preparation
摘要:
A piperidine derivative, which can be used as an intermediate for pharmaceuticals such as paroxetine useful as antidepressants, represented by the general formula (I):
wherein R 1 is hydrogen atom, benzyloxycarbonyl group or tert-butoxycarbonyl group; R 2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position, (3,4-methylenedioxyphenyl)oxymethyl group, carboxyl group or -CO 2 R 7 group in which R 7 is an alkyl group having 1 to 5 carbon atoms, and Z is methylene group or carbonyl group, with proviso that, (A) when R 1 is benzyloxycarbonyl group or tert-butoxycarbonyl group, then R 2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position or (3,4-methylenedioxyphenyl)oxymethyl group, and Z is methylene group; or (B) when R 1 is hydrogen atom and Z is carbonyl group, then R 2 is carboxyl group or -CO 2 R 7 group (R 7 is as defined above); or (C) when R 1 is hydrogen atom and Z is methylene group, then R 2 is hydroxymethyl group.
Also processes for the production of the intermediates are described.
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