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Synfacts 2010(5): 0508-0508  
DOI: 10.1055/s-0029-1219647
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of a Cathepsin S Inhibitor

Contributor(s): Philip Kocienski
J. C. Lorenz*, C. A. Busacca et al.*
Boehringer-Ingelheim Pharmaceuticals, Inc., Ridgefield, USA
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Publication History

Publication Date:
22 April 2010 (online)

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Significance

Cathepsin S is a 24 kD cysteine protease that is implicated in the onset of autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. The target molecule J is a potent, selective, and reversible inhibitor of cathepsin S. The sole stereogenic center in the target molecule was installed by a rhodium-catalyzed asymmetric hydrogenation.