Site-selective 1,3-double functionalization of arenes using para-quinol, C–N, and C–C/C–P three-component coupling

A catalytic and site-selective approach has been demonstrated for dual functionalization of arenes via cross-coupling reactions of p-quinols with amines and isocyanides/phosphites. The strategy enables the production of a series of 3-amino-benzamides and 3-amino-arylphosphonates in good to excellent yields with complete control of regio- and chemo-selectivity. The reaction is highly viable in terms of its environmental benignity, simple operation method, and scalability. Initial mechanistic studies were also carried out to unveil the reaction pathways.