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Synfacts 2008(1): 0004-0004  
DOI: 10.1055/s-2007-992393
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart · New York

Synthesis of Ranirestat (AS-3201)

Contributor(s): Philip Kocienski
T. Mashiko, K. Hara, D. Tanaka, Y. Fujiwara, N. Kumagai*, M. Shibasaki*
The University of Tokyo and Dainippon Sumitomo Pharma Company Ltd., Osaka, Japan
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Publication History

Publication Date:
18 December 2007 (online)

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Significance

Ranirestat is a potent inhibitor of aldose reductase that is in phase III clinical trials for the treatment of diabetic complications. The key step in the synthesis depicted is the efficient asymmetric addition of the β-keto ester A to the azodicarboxylate B catalyzed by ligand C and La(Oi-Pr )3.