The Asymmetric Construction α‐CF₂H Pyrrolidine via 1,3‐Dipolar Cycloaddition of N‐2,2‐Difluoroethylthioisatin Ketoimines with Meldrum's Acid Derived Electron‐Deficient Olefins

Abstract

We report here a directly catalytic asymmetric method in the construction of CF2H‐containing pyrrolidines. A variety of enantioenriched difluoromethylated pyrrolidine (34 examples, up to 97% ee) were obtained on a 1, 3‐dipole cycloaddition model. The subsequent hydrolysis reaction provides a new difluoromethyl substituted fused ring compound which has certain anticancer activity.