Process for the production of etravirine

摘要

A novel process for the preparation of Etravirine comprises the condensing of ethyl cyanoacetate with N-cyanophenylguanidine to obtain an -OH compound of formula (II), which is further converted to a leaving group of formula (III). The compound of formula (III) is optionally protected and brominated to yield compound of formula (IV). The condensation of formula (IV) with 3,5-dimethyl-4-hydroxybenzonitrile yields a compound of formula (VI), and an optional deprotection of the compound of formula (VI) results in Etravirine.