Synthesis of 2-Phosphoryl-3-Monofluorovinylindoles under Catalyst- and Additive-Free Conditions

A synthetic approach for the synthesis 2-phosphoryl-3-monofluorovinylindoles via cascade regioselective dehydrative phosphorylation/stereoselective defluorination of difluoromethylated 3-indolylmethanols and H-phosphine oxides under catalyst- and additive-free conditions is described. The reaction could be scaled-up without the need for column chromatography purification.

Automated summary

A new synthetic approach for the synthesis of 2-phosphoryl-3-monofluorovinylindoles via cascade regioselective dehydrative phosphorylation/stereoselective defluorination is described. The reaction can be scaled-up without the need for column chromatography purification.