Regioselective synthesis of isoquinolinonediones through remote unactivated C(sp³)-H bonds

Herein, a general strategy for the remote-site-selective cascade addition/cyclization of unactivated C(sp(3))-H bonds in free alcohols and sulfonamides to build isoquinolinonedione skeletons is developed. The site selectivity occurs predominantly via a 1,5-hydrogen atom transfer (HAT) process, triggered by heteroatom-centred radicals generated directly under silver catalysis. A broad substrate scope and excellent regio-/chemo-selective control are demonstrated in this method.