作者: Xiaoan Xie , Yu Chen , Dawei Ma
DOI: 10.1021/JA066991J
关键词: Substituent 、 Catalysis 、 Solvent effects 、 Ligand 、 Enantioselective synthesis 、 Molecule 、 Stereoisomerism 、 Coupling reaction 、 Medicinal chemistry 、 Stereochemistry 、 Chemistry
摘要: CuI/trans-4-hydroxy-l-proline-catalyzed coupling reaction of 2-iodotrifluoroacetanilides with 2-methylacetoacetates took place at -45 degrees C to create alpha-aryl all-carbon quaternary centers enantioselectively. Up 93% ee was achieved when tert-butyl ester used. The combination ligand, ortho substituent (participation NHCOCF3), and solvent effects shown account for these unprecedentedly mild conditions.