Patent · US Expired

Process for preparing benzothiazepine derivatives

US5473066A · kind A · utility

2Cited by
0References
6Claims
0Family size

Assignee

Inventors

Key dates

Filing dateJan 19, 1994
Grant dateDec 5, 1995
Priority date
Expiry dateJan 19, 2014

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D281/10
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

Process for stereoselectivity preparing a cis-form of 5-(aminoalkylamino)-1,5-benzothiazepine derivative represented by formula (VI): ##STR1## is provided, said process comprising 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 objective compound (VI).

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.