Process for preparing therapeutically active derivatives of ursodeoxycholic acid.

摘要

Ursodeoxycholic acid derivatives, particularly thioesters, of general formula: <CHEM> wherein R represents -H, -CH3 or -COOH and R1 represents -CONHCH2COOH, -CH2COOH or <CHEM> are active compounds in the treatment of altered biligenetic functions, lithiasis or dyskinesia of biliary ducts. The process according to the invention provides the preparation of the mixed anhydride of ursodeoxycholic acid with alkyl or phenyl chloroformate and its successive reaction with a compound having a -SH group in the chain to form the thioester.