Process for the preparation of gabapentin hydrochloride

Details Process for the preparation of gabapentin hydrochloride Process for the preparation of gabapentin hydrochloride

2006-04-28

2010-02-23

Aulakh, Charanjit S (Department: 1625)

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

Organic compounds

Carboxylic acids and salts thereof

C546S016000, C562S507000

Reexamination Certificate

active

07667071

ABSTRACT:
A process for preparation of gabapentin hydrochloride by converting 1,5-dicyano-2,4-dioxo-3-azaspiro[5,5]-undecane into 1,5-diaminoformyl-2,4-dioxo-3-azaspiro[5,5]-undecane at a temperature of 65° C. to 85° C. in the presence of a strong acid, and then carrying out Hofmann rearrangement under an alkaline condition. The starting material of the process is readily available. The process is simple, and can reduce the purification procedure of intermediates, reduce production cost, and obtain product with higher purity.

REFERENCES:
patent: 6846950 (2005-01-01), Ferrari et al.
patent: 2004/0063997 (2004-04-01), Ferrari et al.
patent: 2247237 (1997-10-01), None
patent: 1109017 (1995-09-01), None
patent: 1471507 (2004-01-01), None
patent: WO-03/002517 (2003-01-01), None
patent: WO-2006/000562 (2006-01-01), None

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