Intercept Pharmaceuticals, Inc.
Methods for the preparation of obeticholic acid and derivatives thereof

Abstract:

The present application relates to a safe method of preparing a bile acid derivative or a pharmaceutical acceptable salt, solvate, or amino acid conjugate thereof, on a large scale from 7-keto lithocholic acid (KLCA), comprising reacting Compound 2 with paraldehyde to form Compound 3 at a temperature between 10.degree. C. and 30.degree. C.: ##STR00001##