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Stereoselective preparation of β,γ-methano-GABA derivatives†‡
David J. Aitken,Ludovic Drouin,Sarah Goretta,Régis Guillot,Jean Ollivier,Marco Spiga
Organic & Biomolecular Chemistry Pub Date : 08/08/2011 00:00:00 , DOI:10.1039/C1OB06095C
Abstract

The Kulinkovich–de Meijere reaction between an unsaturated Grignard reagent and a chiral amide takes place with a high trans stereoselectivity and provides a convenient access to non-racemic trans cyclopropylamines. These compounds are transformed in four steps into the corresponding N-protected β,γ-methano-GABA derivatives, which are obtained for the first time in enantiomerically pure form. The corresponding transformations of the cis cyclopropylamine adducts are also described.

Graphical abstract: Stereoselective preparation of β,γ-methano-GABA derivatives
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