Organocatalytic enantioselective conjugate addition of ketones to isatylidine malononitriles

摘要

An enantioselective Michael addition of ketones to alkylidene-malononitriles catalyzed by chiral primary amine I with (R)-5c as a co-catalyst in good yields (> 90%) and with good enantio-selectivities (85-96% ee) has been developed. The strategy has also been extended to a three-component version through a domino Knoevenagel/Michael sequence with similar or better outcomes.