Synthesis Of Axial Chirality Isoquinoline Compounds Based On C-H Activation Of Iminyl Palladium Intermediates

Nitrogen-containing heterocycles often have important biological activities and play an important role in drug development.Moreover,axially chiral bisaryl scaffold is one of the most important structural units among numerous natural products,bioactive molecules,and functional materials.In asymmetric synthesis,axially chiral biaryl compounds have been widely used as catalysts and ligands.Therefore,the development of new methods to synthesize these compounds has received widespread attention.In this thesis,we developed the Pd-catalyzed reaction of 2-biphenyl isocynide and halogenated compoundsto construct an axially chiral isoquinoline skeleton,via sequential oxidative addition,migration insertion,C-H activation steps.This reaction provides Quinap and Phenap analouges in a simple manner.The preliminary screening of several commonly used chiral ligands showed that controlling of enantioselectivity faces significant challenge.