Process for the synthesis of pregabalin

Details Process for the synthesis of pregabalin Process for the synthesis of pregabalin

2010-04-29

2011-11-22

Zucker, Paul A (Department: 1621)

Organic compounds -- part of the class 532-570 series

Organic compounds

Carboxylic acids and salts thereof

C562S606000

Reexamination Certificate

active

08063244

ABSTRACT:
A process for the preparation of a compound of formula (I) is disclosed,which comprises:a) the reaction of a compound of formula (II)with zinc azide of formula (III)in-line-formulae description="In-line Formulae" end="lead"?Zn(N3)2  (III)in-line-formulae description="In-line Formulae" end="tail"?in the presence of a solvent of formula R1—OH, wherein R1is herein defined, to obtain a compound of formula (IV),b) its conversion into a compound of formula (V);c) its enantiomeric enrichment to obtain the (S) enantiomer of formula (VI); andd) the hydrolysis thereof.

REFERENCES:
patent: 5637767 (1997-06-01), Grote
patent: 6197819 (2001-03-01), Silverman
patent: 6359169 (2002-03-01), Silverman
patent: 2005/0283023 (2005-12-01), Hu
patent: 1992609 (2008-11-01), None
patent: WO 2008/009897 (2008-01-01), None
Hoekstra et al., “Chemical Development of CI-1008, an Enantiomerically Pure Anticonvulsant”, Organic Process Research & Development, 1997, 1: pp. 26-38.

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