Intercept Pharmaceuticals, Inc.
Methods and intermediates for the preparation bile acid derivatives

Abstract:

The present invention relates to methods and novel intermediates useful in the preparation of a compound of formula (A) ##STR00001## or a pharmaceutically acceptable salt thereof, comprising converting the aldehyde of a compound of formula (B) with a reducing agent to prepare a compound of formula (C) ##STR00002## and converting the compound of formula (C) with a sulfating reagent to prepare a compound of formula (A). An objective of the present invention is to provide methods of preparing bile acid derivatives and novel intermediates. A use of the methods and intermediates described relates to the synthesis of bile acid derivatives which activate both FXR and TGR5.