2-Position-selective CH fluoromethylation of six-membered heteroaryl N-oxides with (fluoromethyl)triphenylphosphonium iodide

Abstract A mild and efficient method for the regioselective C H fluoromethylation of heteroaryl N-oxides with (fluoromethyl)triphenylphosphonium iodide is presented. With LiOt-Bu as the base and DMSO as the solvent, this reaction delivers a series of C2-fluoromethylated pyridine and quinoline derivatives in moderate to good yields. This protocol also extends the synthetic applications of (fluoromethyl)triphenylphosphonium iodide.