A PROCESS FOR THE PREPARATION OF ILOPERIDONE AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF

摘要

The present invention relates to a new process for the preparation of 1- [4-[3-[4-(6-fluoro- 1,2-benzisoxazol-3-yl)- l-piperidinyl]propoxy]-3- methoxyphenyl]- ethanone (Iloperidone) and salts thereof. The synthetic process comprises the reaction between itself 6-fluoro-3-(4- piperidinyl)-l,2-benzisoxazole of formula II as base rather than use of its hydrochloride as mostly reported in prior art and l-[4-(3- chloropropoxy)-3-methoxyphenyl]ethanone of formula III. This invention also relates to a process for the preparation of carbonated iloperidone; an impurity of the formula IV formed during the condensation of the compound of formula II and compound of formula III in presence of a base, method of its isolation and characterization thereof, as well as its use as a reference standard and reference marker in analytical department while evaluating the purity profile of iloperidone. Formula (I) (II) (III)