Asymmetric synthesis of a potent azepanone-based inhibitor of the cysteine protease cathepsin K |
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Authors: | Robert E. Lee Trout |
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Affiliation: | Department of Medicinal Chemistry, Microbial, Musculoskeletal and Proliferative Diseases, GlaxoSmithKline, Collegeville, PA 19426, USA |
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Abstract: | In this account we detail the asymmetric synthesis of 1, a potent azepanone-based inhibitor of cathepsin K (Ki = 0.16 nM), which has been shown to inhibit the production of biomarkers of bone resorption in monkeys. The key steps in the synthesis sequence were the utility of the Evans aldol reaction coupled with the ring closing olefin metatheses to assemble the azepanone core contained within 1. |
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Keywords: | Asymmetric synthesis Aldol Ring closing olefin metatheses |
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