Visible-Light-Induced Highly Site-Selective Direct C–H Phosphorylation of Pyrrolo2,3-dpyrimidine Derivatives with H-Phosphine Oxides

An efficient and highly regioselective C6-phosphorylation protocol for pyrrolo2,3-dpyrimidine (7-DAP) derivatives with various H-phosphine oxides induced by visible light at room temperature is described for the first time. This protocol has been successfully achieved by the combination of Na2-eosin Y as a photocatalyst and LPO as an oxidant under transition metal- and additive-free conditions. The broad substrate scope, good functional group tolerance, excellent regioselectivity, and air tolerant conditions make this process favorable for the functional modification of pyrrolo2,3-dpyrimidine scaffold and enrich the phosphorylated 7-DAP compounds for further biological evaluation.