4,5-Disubstituted cis-pyrrolidinones as inhibitors of 17beta-hydroxysteroid dehydrogenase II.Part 1:Synthetic approach

摘要

17beta-Hydroxysteroid dehydrogenase II (17beta-HSD II) antagonists may provide an important way into preventing the onset of osteoporosis.The discovery of 4,5-disubstituted cis-pyrrolidinones as 17beta-HSD II inhibitors led to the development of an efficient intramolecular Michael addition,followed by catalytic hydrogenation to obtain the desired cis configuration.