Intercept Pharmaceuticals, Inc.

Kayla R Iorga

Kevin Schaab

Paul E Whitley

Flavio Chavez Lopez

The present invention relates to methods and novel intermediates useful in the preparation of a compound of formula (A) 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) 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.

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Dalzell, SC, United States of America

Kayla R Iorga