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Synfacts 2006(3): 0188-0188
DOI: 10.1055/s-2006-931946
DOI: 10.1055/s-2006-931946
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart · New YorkSynthesis of an Apical Sodium-Codependent Bile Acid Transporter Inhibitor
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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Publikationsverlauf
Publikationsdatum:
21. Februar 2006 (online)
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.