4,5-Disubstituted cis-pyrrolidinones as inhibitors of 17β-hydroxysteroid dehydrogenase II. Part 1: Synthetic approach |
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| Authors: | James H. Cook,Jeremy Barzya,Catherine Brennan,Derek Lowe,Yamin Wang,Anikó Redman,William J. Scott,Jill E. Wood |
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| Affiliation: | Department of Chemistry Research, Bayer Research Center, 400 Morgan Lane, West Haven, CT 06516, USA |
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| Abstract: | 17β-Hydroxysteroid dehydrogenase II (17β-HSD II) antagonists may provide an important way into preventing the onset of osteoporosis. The discovery of 4,5-disubstituted cis-pyrrolidinones as 17β-HSD II inhibitors led to the development of an efficient intramolecular Michael addition, followed by catalytic hydrogenation to obtain the desired cis configuration. |
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| Keywords: | Hydroxysteroid dehydrogenase Intramolecular Michael addition 4,5-Disubstituted pyrrolidinones |
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