Patent ID: 7678902
Filing Date: 2010-03-16
Classification: A61P,C07D

Abstract:
1. A process for the preparation of 11-(4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl)-dibenzo[b,f][1,4]thiazepine expressed by Formula 1, comprising the following steps of: (a) reacting 2,2′-dithiosalicylic acid which is expressed by Formula 5 with 1-chloro-2-nitrobenzene in a basic aqueous solution in the presence of or in the absence of a reducing agent, to produce 2-(2-nitrophenylthio)benzoic acid expressed by Formula 6; (b) reducing a nitro group of 2-(2-nitrophenylthio)benzoic acid which is expressed by Formula 6 in the presence of hydrogen and a solvent under a heterogeneous metal catalyst, to produce 2-(2-aminophenylthio)benzoic acid expressed by Formula 7; (c) simultaneously conducting cyclization and chlorination reactions of 2-(2-aminophenylthio)benzoic acid which is expressed by Formula 7 in an organic solvent in the presence of a halogenating agent and a base, and continuously reacting a resulting compound with piperazine without separation, to produce 11-piperazinyl-dibenzo[b,f][1,4]thiazepine expressed by Formula 4; and (d) reacting 11-piperazinyl-dibenzo[b,f][1,4]thiazepine which is expressed by Formula 4 with 2-haloethoxyethanol in an organic solvent under a base, to produce 11-(4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl)-dibenzo[b,f][1,4]thiazepine expressed by Formula 1