Hydro-de-halogenation and consecutive deprotection of chlorinated N-amido-pyrrolidin-2-ones with Raney-Ni:: an effective approach to gabapentin

被引：24

作者：

Cagnoli, R

Ghelfi, F

Pagnoni, UM

Parsons, AF

Schenetti, L

机构：

[1] Univ Modena & Reggio Emilia, Dipartimento Chim, I-41100 Modena, Italy

[2] Univ York, Dept Chem, York YO10 5DD, N Yorkshire, England

来源：

TETRAHEDRON | 2003年 / 59卷 / 50期

关键词：

hydrazides; cyclizations; pyrrolidinones; hydrogenolysis;

D O I：

10.1016/j.tet.2003.10.046

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The benzoylamino group was identified as a useful radical cyclization auxiliary that can be smoothly removed on hydro-dehalogenation of chlorinated N-substituted-pyrrolidin-2-ones with Raney-Ni. This methodology was successfully implemented in a new and appealing route to the anti-epileptic drug gabapentin. (C) 2003 Published by Elsevier Ltd.

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收藏

页码：9951 / 9960

页数：10

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