Asymmetric Three-component Cyclization/Mannich Tandem Reaction Involving O-Alkynylbenzaldehyde,Aniline And Diazophosphonate

In this paper,a series of chiral Br?nsted acid ligands were designed and synthesized,which reacted with metal salts to form complexes.They were used to catalyze the three-component asymmetric cyclization/Mannich series reaction of o-alkynylbenzaldehyde,aniline and diazophosphonate,and the chiral 1,2-dihydroisoquinoline compounds were synthesized.By optimizing the reaction conditions,the target product can be obtained with excellent yields(up to 97%)and enantioselectivities(up to 98%).The reaction has the advantages of mild conditions,easy recovery of catalyst,wide application range of substrates and high atom economy.These reactions also provide a novel method for the synthesis of chiral 1,2-dihydroisoquinoline compounds.