文摘
An efficient method for the CF<sub>3sub>-carbenoid C-7 functionalization of N-pyrimidylindolines has been developed. This protocol uses readily available methyl 3,3,3-trifluoro-2-diazopropionate as a cross-coupling partner and smoothly proceeds under chelation-controlled Rh<sup>IIIsup> catalysis. The reactions provide the indoline products with high regioselectivity within a few hours and allow for the introduction of both the CF<sub>3sub> and carboxylate functions at the C-7 position.