A PROCESS FOR THE PREPARATION OF 2-[2-(4-DIBENZO[b,f] [L,4] THIAZEPIN-11-yl-1- PIPERAZINYL)ETHOXY] ETHANOL FUMARATE

摘要

A process for the preparation of 2-[2-(4-Dibenzo[b,f] [l,4] thiazepin-11-yl-1- ?iperazinyl)ethoxy] ethanol fumarate commonly known as Quetiapine hemifumarate. Dibenzo[b,f] [l,4] thiazepin-11-[10H]one is halogenated with a halogenating agent in the ratio of 1 : 0.5 to 3 w/v in an organic solvent in the presence of an organic base at reflux temperature followed by condensation of the reaction with piperazine without isolating the imino chloride. The piperazinyl-dibenzo[b,f] [l,4] thiazepine is converted to Quetiapine hemifumarate which is purified by crystallization with alcohol at reflux temperature and precipitated it by cooling the reaction mixture and recovered by filtration.