DRUG SYNTHESIS METHODS AND MANUFACTURING TECHNOLOGY A NEW PREPARATIVE METHOD FOR THE SYNTHESIS OF 6-(3-(1-ADAMANTYL)-4-METHOXYPHENYL)-2-NAPHTHOIC ACID

摘要

A new method for the synthesis of 6-[3-(l-adamantyl)-4-methoxyphenyl]-2-naphthoic acid (adapalene) was developed, characterized by stable high yields of intermediate and end products, simple scale-up, and technical feasibility.6-[3-(1-Adamantyl)-4-methoxyphenyl]-2-naphthoic acid (I) is an active pharmaceutical ingredient whose international non-proprietary name is adapalene. This compound is an atypical synthetic retinoid and is widely used in dermatology as an effective agent for the treatment of acne [1]. Compound I binds to nuclear retinoic acid receptors (RARs) and affects cell differentiation and inflammation processes.