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Synfacts 2010(5): 0508-0508
DOI: 10.1055/s-0029-1219647
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
J. C. Lorenz*, C. A. Busacca et al.*
Boehringer-Ingelheim Pharmaceuticals, Inc., Ridgefield, USA
Further Information
Publication History
Publication Date:
22 April 2010 (online)
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.