Method for preparing Adapalene

Abstract

A process for preparing adapalene features the hydrolyzing reaction between 6[3-(1-adamantyl)-4methoxyphenyl]-2-methyl naphthanleneformate and one or more of potassium hydroxide, ammonia water and potassium carbonate in polar solvent.

Description

technical field [0001] The invention relates to a preparation method for adapalene obtained from alkaline hydrolysis of methyl 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoate in a polar solvent. Background technique [0002] Adapalene (adapalene), chemical name 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid, is an aryl propionic acid derivative, a new naphthalene Formic acid derivatives, belonging to the third generation of retinoic acid drugs, are selective β-retinoic acid receptor agonists, and are clinically used to treat acne and psoriasis. At present, foreign countries have industrialized production, and my country basically relies on imports, only a small amount of self-production, but the cost is relatively high, and the three wastes are serious. Document US4717720 reports the laboratory synthesis of adapalene, using sodium and methanol to prepare sodium methoxide for hydrolysis, the yield is 78%, but industrial production is difficult, and the cost is high, t...

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Problems solved by technology

Document US4717720 reports the laboratory synthesis of adapalene, using sodium and methanol to prepare sodium methoxide for hydrolysis, the yield is 78%, but industrial production is difficult, and the cost is high, the three wastes are serious, and resource consumption

Another document (Chinese Journal of Pharmaceutical Industry, 2005, 36 (12) the synthesis of adapalene) reports that 95% methanol using sodium hydroxide is hydrolyzed, but the yield is 51%

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