Highly‐Selective Construction of Aza‐Fused Pyrrolo Isoquinoline Derivatives

Abstract A novel Rh(III)‐catalyzed cascade C−H activation/annulation/nucleophilic attack/Michael addition of 2‐phenyloxazoles with maleimides for highly‐selective construction of pyrroloisoquinoline derivatives through conditions control is reported. In this reaction, oxazoles were used both as the directing group and potential functionalized reagents, H 2 O was the nucleophile. The notable features of this protocol include atom economy and highly regioselectivity.