The Practical Synthesis of Double Axial Chiral Guanidines

Two novel double axial chiral guanidines were designed according to the concept of double axial chirality. The practical synthetic procedures from (S)-1,1'-binaphthol have been developed. The title compounds were fully characterized by NMR, MS, IR and elemental analysis or HRMS. The two chiral guanidines can be interesting catalysts for asymmetric catalysis and preliminary asymmetric catalytic activity was investigated in Henry reaction and conjugate addition.