Palladium‐Catalyzed Olefination of 4H‐Benzo[d][1,3]oxazin‐4‐one Derivatives with Activated Alkenes via Preferential Cyclic Imine‐N‐Directed Aryl C‐H Activation

Abstract

A palladium‐catalyzed chelation‐assisted selective ortho C‐H bond olefination of biologically active 4H‐benzo[ d ][1,3] oxazin‐4‐one derivatives with activated olefins has been achieved. The products are obtained in good yields with high regio‐ and stereoselectivities. This new protocol has been demonstrated to provide a variety of olefinated‐4H‐benzo[d][1,3]oxazin‐4‐one derivatives. The site selectivity of the reaction was explained by a DFT study.