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US 7,888,511 B2Granted
Method of preparing esomeprazole and salts thereof
AssigneeHanmi Holdings Co., Ltd.
InventorsTae Hee Ha, Won Jeong Kim, Hee Sook Oh, Chang Hee Park, Jae Chul Lee, Han Kyong Kim, Kwee-Hyun Suh
Life of this patent
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Abstract
Optically pure esomeprazole and its salt can be simply prepared by dissolving (S)-(−)-binol, a weak base and the racemic form of omeprazole in a mixture of a water-compatible organic solvent and water at a high temperature, cooling the mixed solution to crystallize the inclusion complex of esomeprazole and (S)-(−)-binol, and removing the (S)-(−)-binol moiety from the crystallized inclusion complex.
Claims14
A method of preparing esomeprazole of formula (II) or its salt having an optical purity of at least 98% ee, which comprises:
- (A) dissolving (S)-(−)-binol, a weak base and the racemic form of omeprazole in a mixture of a water-compatible organic solvent and water at a temperature ranging from 30 to 70° C., and cooling the resulting solution to a temperature of −5° C. to room temperature to allow the crystallization of the inclusion complex of esomeprazole and (S)-(−)-binol of formula (I);
- and
- (B) removing the (S)-(−)-binol moiety from the inclusion complex of formula (I) obtained in step (A) by filtration or extraction:
Dependencies are inferred from the claim text.