Cinchona Alkaloid/TiIV‐Catalyzed Enantioselective Enamine–Trifluoropyruvate Condensation–Cyclization Reaction and Its Application to Drug‐like Heterocycles

Drug design: A cinchona alkaloid/TiIV-catalyzed enantioselective tandem enamine–trifluoropyruvate condensation–cyclization reaction provides a robust method for the construction of small heterocyclic molecules with a quaternary trifluoromethylated carbon center (see scheme). The series of products are attractive templates and were readily converted to drug-like trifluoromethylated heterocycles by conventional methods.