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Synfacts 2011(12): 1280-1280  
DOI: 10.1055/s-0031-1289319
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of TAK-475

Contributor(s): Philip Kocienski
M. Goto*, T. Konishi, S. Kawaguchi, M. Yamada, T. Nagata, M. Yamano
Takeda Pharmaceutical Co. Ltd., Yamaguchi and Takeda Pharmaceutical Co. Ltd., Osaka, Japan
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Publication History

Publication Date:
18 November 2011 (online)

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Significance

TAK-475 is a squalene synthase inhibitor that was a lead for the lowering of plasma cholesterol. This paper focuses on a single step; the asymmetric hydrogenation of the benzophenone A to the benzhydrol C. A new variant B of Noyori’s BINAP precatalyst enabled efficient asymmetric hydrogenation of the prochiral benzophenone A with high er (97:3) under low pressure (<1 MPa).