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[3+2] Cycloaddition of Arynes with CF3CHN2 for the Synthesis of 3-Trifluoromethyl-1H-indazoles
Ma et al. have reported the efficient [3 + 2] cycloaddition reactions of arynes with CF3CHN2 for the synthesis of 3-trifluoromethyl-1H-indazoles. According to their results, arynes in situ generated from 2-(trimethylsilyl)phenyl triflate by treatment with CsF react with CF3CHN2 in the presence of TEBAC under mild conditions to afford the corresponding 3-trifluoromethyl-1H-indazole derivatives in high yields. Since 3-trifluoromethylindazoles are useful because of their potential biological activities, this reaction is expected to be an experimentally simple synthetic method for those compounds.