The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Dec. 25, 2012

Filed:

May. 22, 2008
Applicants:

Donna D. Yu, Arcadia, CA (US);

Barry M. Forman, Irvine, CA (US);

Inventors:

Donna D. Yu, Arcadia, CA (US);

Barry M. Forman, Irvine, CA (US);

Assignee:

City of Hope, Duarte, CA (US);

Attorneys:
Primary Examiner:
Int. Cl.
CPC ...
C07J 17/00 (2006.01); C07J 9/00 (2006.01);
U.S. Cl.
CPC ...
Abstract

A novel, improved method of synthesizing alkylated bile acid derivatives is provided. Such derivatives include, but are not limited to the active, potent, and selective FXR receptor agonist such as 6-ECDCA and other CA, DCA and CDCA derivatives. The first step of the synthesis selectively oxidates CDCA, CD, or DCA related starting material. An efficient combined deprotonation, trapping, ethylation, deprotection and reduction system is used to produce the desired alkylated bile acid derivatives. This practical synthesis offers a simple and economical pathway suitable for a large-scale manufacturing of alkylated bile acid derivatives including, but not limited to, 6-ECDCA.


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