Synthesis of enantiopure 3,4-disubstituted piperidines. An asymmetric synthesis of (+)-paroxetine

被引:31
作者
Amat, M
Hidalgo, J
Bosch, J
机构
[1] Laboratory of Organic Chemistry, Faculty of Pharmacy, University of Barcelona
关键词
D O I
10.1016/0957-4166(96)00189-9
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
An asymmetric synthesis of the 3,4-trans-disubstituted piperidine derivative (+)-paroxetine from the chiral non racemic lactam 1 is reported. The p-fluorophenyl substituent is introduced by conjugate addition to the unsaturated lactams 3 whereas the aryloxymethyl substituent at the 3-position is assembled by taking advantage of the activating alkoxycarbonyl group of 3. (C) 1996 Elsevier Science Ltd
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页码:1591 / 1594
页数:4
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