Method for preparing Adapalene

An equation and reaction technology, applied in the preparation of carboxylate/lactone, organic chemistry, etc., can solve the problems of resource consumption, serious three wastes, and high cost, and achieve the effect of reducing costs, reducing resource consumption, and reducing three wastes
CN1830937AInactive Publication Date: 2006-09-13JIANGSU ZHONGDAN GROUP +2

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
JIANGSU ZHONGDAN GROUP
Publication Date
2006-09-13
Estimated Expiration
Not applicable · inactive patent

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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.
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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...

Claims

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