Zhao Group
School of Chemical Biology & Biotechnology

Palladium-Catalyzed Benzo[d]isoxazole Synthesis by C-H Activation/[4+1] Annulation


Recently, our group has reported a palladium-catalyzed intermolecular [4+1] annulation of N-phenoxyacetamides with aldehydes to form 1,2-benzisoxazoles. By activating the C-H bonds ortho to phenol-derived O-N bonds, the method enables the simultaneous construction of C-C and C=N bonds in 1,2-benzisoxazoles with the O-N bonds intact. The method has been successfully applied to the synthesis of the active pharmaceutical intermediates, such as risperidone. This work has been finished by Pingping Duan and has been published on Chemical Science, named "Palladium-Catalyzed Benzo[d]isoxazole Synthesis by C-H Activation/[4+1] Annulation".