METHOD FOR PRODUCING 11-AMINO-3-CHLORO-6,11-DIHYDRO-5,5- DIOXO-6-METHYL-DIBENZOc,f 1,2THIAZEPINE AND APPLICATION THEREOF TO SYNTHESIS OF THIANEPTINE

摘要

PROBLEM TO BE SOLVED: To provide a method for producing 11-amino-3-chloro-6,11-dihydro-5,5- dioxo-6-methyl-dibenzo[c,f] [1,2]thiazepine by using a starting material having no problem in the maximum yield and purity, and capable of being readily changed to an industrial scale. SOLUTION: This method is characterized in that the objective compound is obtained by reacting a ketone of formula (III) with sodium borohydride in the presence of a two-phase medium (e.g. chloroform), treating the product with hydrogen chloride to provide a chloride, and further treating the resultant chloride with ammonia, and the obtained compound is optionally converted to an additional salt such as a hydrochloride.