Cu(ii)-catalyzed ‘in-water’ N-arylation of electron-deficient NH-heterocycles

Abstract

Cu(II)-catalyzed N-arylation of electron-deficient NH-heterocycles ‘in-water’ at room temperature is described. A wide substrate scope with respect to structural and electronic variation of NH-heterocycles plus arylboronic acids allows product diversity. The functional group tolerance, ‘gram-scale’ synthesis, synthetic elaboration of N-arylated products and late-stage arylation are the distinct advantages.