RhIII-Catalyzed C–H Heteroarylation and C–N Cleavage: Direct Access to C2-heteroarylated (NH)-indoles

Key Points

• The aim is to develop a method for C2-heteroarylation of indoles and subsequent cleavage of the amide auxiliary.
• Utilized Cp*Rh(III) as a catalyst for the reaction
• Incorporated N 2,6 difluoroaryl amide auxiliary to assist the reaction
• Applied heterocyclic boronates for the heteroarylation step
• Conducted auxiliary cleavage to obtain biheteroaryl derivatives
• Successful C2-heteroarylation of indoles was achieved
• Efficient auxiliary cleavage provided access to complex biheteroaryl derivatives
• Demonstrated high yields in the synthesis process