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Generated: September 24, 2017

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Title:Preparation of bile acids and intermediates thereof
Abstract: Synthetic methods for preparing deoxycholic acid and intermediates thereof are provided.
Inventor(s): Prasad; Achampeta Rathan (Hyderabad, IN), Swaringen, Jr.; Roy A. (Durham, NC), Reid; John Gregory (Groton, MA), Moriarty; Robert M. (Michiana Shores, IN), Sahoo; Akhila Kumar (Hyderabad, IN)
Filing Date:Dec 28, 2012
Application Number:13/730,533
Claims:1. A method of preparing a compound of formula 1.7: ##STR00029## comprising reacting a compound of formula 1.6: ##STR00030## with an alkylpropiolate HC.ident.CC(O)OR or an alkyl acrylate CH.sub.2.dbd.CHC(O)OR wherein R is alkyl in the presence of a Lewis acid to form a compound of formula 1.7 wherein P is a protecting group, R is a alkyl, and the dashed line ---- is a single or double bond, to provide the compound of formula 1.7.

2. The method of claim 1 wherein the Lewis acid is EtCl.sub.2.

3. The method of claim 1 wherein the alkylpropiolate or alkylacrylate is methylpropriolate or methylacrylate.

4. A method of preparing a compound of formula 2.1: ##STR00031## comprising reacting a compound of formula 2.0 ##STR00032## with a reducing agent to form a compound of formula 2.1 wherein P is a protecting group and R is alkyl, to provide a compound of formula 2.1.

5. The method of claim 4 wherein the reducing agent is LiAl(OtBu).sub.3H.
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Argus Health
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Cantor Fitzgerald
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