Synthesis of isoquinolinones via regioselective palladium-catalyzed C–H activation/annulation

The isoquinoline motif and its derivatives are of significant interest due to their important biological activities. The effective synthesis of substituted isoquinoline compounds has historically been a significant challenge. A new palladium-catalyzed C–H activation/annulation of N-methoxy benzamides and 2,3-allenoic acid esters is described. For the first time, 2,3-allenoic acid esters are employed for the syntheses of 3,4-substituted hydroisoquinolones, the heteroannulation of allenes proceeded smoothly and afforded the products with good yields and excellent regioselectivity.