PROCESS FOR PREPARING BENZOTHIAZEPINE DERIVATIVES

摘要

The present invention is directed to a process for stereoselectivity preparing a cis-form of 5-(aminoalkylamino)-1,5-benzothiazepine derivative represented by formula (VI): <IMG> (VI) which comprises carrying out a stereoselective addition reaction of an o-(aminoalkylamino)thiophenyl derivative with a trans-substituted glycidic ester at an elevated temperature in a nonpolar solvent in the presence of a divalent or trivalent iron ion to prepare a threo-form intermediate, hydrolyzing the ester group of said intermediate, acetylating the hydroxyl group of said hydrolyzed compound, and subjecting said acetylated compound to a ring closure reaction to obtain the desired compound (VI). The compounds of the formula (VI) are useful as pharmaceutical compounds with vasodilation action and cardiac-muscle protecting action.