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Synfacts 2006(3): 0188-0188  
DOI: 10.1055/s-2006-931946
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart · New York

Synthesis of an Apical Sodium-Codependent Bile Acid Transporter Inhibitor

Contributor(s): Philip Kocienski
H.-C. Huang*, S. J. Tremont*
Pharmacia, Chesterfield and Creve Coeur, Missouri; Pharmacia, Skokie, Illinois; University of Missouri, St. Louis, USA
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Publication History

Publication Date:
21 February 2006 (online)

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Significance

An extensive analogue program identified benzothiepine I as a potent, crystalline, nonhygroscopic apical sodium-codependent bile acid transporter (ASBT) inhibitor as a potential drug for lowering serum LDL cholesterol. A remarkable step is the highly enantio- and diaste­reoselective ring closure of the aldehyde derived from F to benzothiepine G.