Visible-Light Induced Iron-Catalyzed Hydroxymethylation of N-Heterocycles
A new strategy for iron-catalyzed visible-light induced hydroxymethylation of N-heterocycles with methanol under mild conditions was developed.By employing FeCl3 as the catalyst,2-methylisonicotinic acid as the ligand,TsOH as the acid,air as the oxidant,and aqueous MeOH as the solvent,varieties of substituted quinolines,isoquinolines,pyridines,benzothia-zole and voriconazole were hydroxymethylated smoothly in good to excellent yields,exhibiting good substrate scope.This strategy features green reaction conditions,excellent atom-economy and simple operations.It has potential applicable value in late-stage structure modification of drug molecule.
iron catalysishydroxymethylationvisible-light catalysisN-heterocycle
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