Enantioselective Mannich-Type Reactions to Construct Trifluoro-methylthio-Containing Tetrasubstituted Carbon Stereocenters via Asymmetric Dual-Reagent Catalysis

摘要

An approach to construct tetrasubstituted carbon stereocenters bearing both a trifluoromethylthio (SCF3) group and a cyano group has been realized, through asymmetric organophosphine-catalyzed Mannich-type reactions. The products were obtained in high yields and moderate to high enantiose-lectivities. Two diastereoisomers could be isolated from each reaction (overall 25 examples), rendering this approach a viable opportunity for molecular diversity generation and improvement of the bioactivity of related drug candidates.