An efficient method to access 2-fluoroalkylbenzimidazoles by PIDA oxidation of amidines

A mild and practical strategy for the synthesis of 2-bromodifluoromethyl (or trifluoromethyl)-1H-benzimidazoles via PIDA-mediated oxidative intramolecular cyclization of the fluorinated amidines is described. The approach has the advantages of superior yields, excellent functional groups tolerance and mild reaction conditions.

. A mild and practical strategy for the synthesis of 2-bromodifluoromethyl (or trifluoromethyl)-1H-benzimidazoles via PIDA-mediated oxidative intramolecular cyclization of the fluorinated amidines is described. The approach has the advantages of superior yields, excellent functional groups tolerance and mild reaction conditions.Figure optionsDownload as PowerPoint slideHighlights
► Synthesis of 2-bromodifluoromethyl (trifluoromethyl)-1H-benzimidazoles is described.
► Intramolecular cyclization of the fluorinated amidines via PIDA-mediated is used.
► The approach tolerates more functional groups than non-fluorinated counterparts.