Process for preparing benzothiazepine derivatives

Details Process for preparing benzothiazepine derivatives Process for preparing benzothiazepine derivatives

C - Chemistry, Metallurgy

07

C

C07C 323/63 (2006.01) C07C 319/14 (2006.01) C07C 323/56 (2006.01) C07D 207/34 (2006.01) C07D 213/74 (2006.01) C07D 231/38 (2006.01) C07D 233/88 (2006.01) C07D 239/42 (2006.01) C07D 281/10 (2006.01) C07D 295/13 (2006.01) C07D 295/155 (2006.01) C07D 417/06 (2006.01)

Patent

CA 2114036

Abstract 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): Image (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. - 1 -

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