Organocatalytic Asymmetric Michael Reaction of Cyclic 1,3-Dicarbonyl Compounds and α,β-Unsaturated Ketones-A Highly Atom-Economic Catalytic One-Step Formation of Optically Active Warfarin Anticoiagulant

摘要

As optically active drugs become increasingly important for the treatment of diseases in patients, still more enantiopure drugs are introduced to the market either as new drugs or as the result of a racemic switch. An important goal for asymmetric catalysis is to develop new reactions that afford optically active compounds from simple and easily available starting materials and catalysts. However, the ultimate goal would be if the new reaction could be used directly for a one-step synthesis of optically active molecules that have important biological and pharmaceutical activities. Herein we present such as advance and its direct application in an atom-economic synthesis of optically active drugs based on the development of a new organocatalytic enantioselective Michael addition of cyclic 1,3-dicarbonyl compounds to α,β-unsaturated ketones.