Patent ID: 6653492
Filing Date: 2003-11-25
Classification: C07J

Abstract:
A method of producing lithocholic acid of formula (I) or an optionally substituted derivative thereof which comprises:a) hydrogenating ethyl-3-oxo-4, 22-choladienate of Formula (II) or an optionally substituted derivative thereof in the presence of a catalyst â€ƒto give ethyl-3-oxocholanate of Formula (III) or the corresponding substituted derivative thereof: â€ƒfollowed by: b) hydrolyzing the C-24 ester group of the intermediate of formula (III) obtained in step a), or the corresponding substituted derivative thereof, to give 3-oxocholinic acid of Formula (IV) or the corresponding substituted derivative thereof, â€ƒand reduction of the 3-keto group of this intermediate to give lithocholic acid of Formula (I) or the corresponding substituted derivative thereof, â€ƒor alternatively, c) reducing the 3-ketogroup of the intermediate (III), obtained in step a), or the corresponding substituted derivative thereof, to give the intermediate of formula (V): â€ƒfollowed by hydrolysis of the C-24 ester group to give lithocholic acid of Formula (I) or the corresponding substituted derivative thereof.