Organocatalytic asymmetric synthesis of benzothiazolopyrimidines via a [4 + 2] cycloaddition of azlactones with 2-benzothiazolimines

A chiral guanidine-catalyzed [4 + 2] cycloaddition of 2-benzothiazolimines with azlactones characterized by a high yield, ee, and dr and a broad substrate scope has been developed. Gram-scale synthesis and derivatization of the product revealed the potential of utility.