4.4 Article

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

期刊

TETRAHEDRON
卷 59, 期 50, 页码 9951-9960

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tet.2003.10.046

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hydrazides; cyclizations; pyrrolidinones; hydrogenolysis

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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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