Feng-Yan Ge, Zengxue Wang, W. Wan
Apr 30, 2007
Citations
0
Influential Citations
43
Citations
Journal
Tetrahedron Letters
Abstract
2-Trifluoromethyl and 2-difluoromethyl substituted benzimidazole, benzoxazole and benzothiazole derivatives were efficiently prepared through a one-pot reaction of trifluoroacetic acid and difluoroacetic acid, respectively, with commercially available o-phenylenediamines, 2-aminophenols, and 2-aminobenzenethiols in good to excellent yields. Subsequential bromination of 2-difluoromethyl groups by photolysis with NBS led to the formation of bromodifluoromethyl benzo-1,3-diazoles which may be utilized to prepare the new generation of gem-difluoromethylene linked identical or non-identical twin molecules for drug synthesis.