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US 6,441,226 B1Granted
Process for the preparation of isotretinoin
AssigneeRanbaxy Laboratories Limited
InventorsMohammad Salman, Vijay Kumar Kaul, J. Suresh Babu, Naresh Kumar
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Abstract
The present invention relates to a process for the preparation of 13-cis isomer of Vitamin A acid, commonly known as isotretinoin, in a single step.
Claims9
A process for the preparation of isotretinoin in a single step, which comprises:
- condensation of dienolate of methyl 3,3-dimethyl acrylate of Formula I:
- with β-ionylidene-acetaldehyde of Formula II:
- in a suitable solvent at a temperature between −60° C. to −80° C. for 1-2 hours to produce the intermediate lactone of Formula III, and
- raising temperature of the reaction mixture to 25° C. to 45° C. and stirring for 1-24 hours;
- followed by aqueous acidic work up to form isotretinoin of Formula IV:
- containing less than 0.1% of tretinoin impurity of Formula V:
3 more elements
Dependencies are inferred from the claim text.