Cu(Ⅰ)-Catalyzed asymmetric exo-selective synthesis of substituted pyrrolidines via a 1,3-dipolar cycloaddition reaction

摘要

An (R)-DM-BINAP/Cu(CH_3CN)_4BF_4 complex catalyzed exo-selec-tive asymmetric 1,3-dipolar cycloaddition (1,3-DCA) reaction of imino esters with α,β-unsaturated pyrazoleamides has been developed. A series of highly functionalized pyrrolidines with multiple stereogenic centers were obtained with good yields and diastereoselectivities and excellent enantioselectivities (up to 99% ee).