Cinchona alkaloid/TiIV-catalyzed enantioselective enaminetrifluoropyruvate condensation-cyclization reaction and its application to drug-like heterocycles

Abstract

(Chemical equation presented) Drug design: A cinchona alkaloid/Ti IVcatalyzed 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. © 2010 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.