Regioselective synthesis of 3,4-disubstituted isocoumarins through the Pd-catalyzed annulation of 2-iodoaromatic acids with ynamides†
Abstract
A Pd(0)-catalyzed annulation reaction of ynamides is described for the efficient synthesis of 3,4-disubstituted isocoumarins. This novel methodology allows for the concomitant construction of O–C and C–C bonds between 2-iodoaromatic acids and ynamides, exhibiting excellent regioselectivities and a wide functional group tolerance.