Abstract
A method for the synthesis of 2-borylindoles via copper(I)-catalyzed borylative cyclization of 2-alkenylphenyl isocyanides with B2pin2 is presented. The reaction is tolerant of functional groups, such as Br, CN and CO2R; however, the resulting pinacolboranes are sensitive to column chromatography (yields after NMR analysis are given). After filtration and evaporation of the solvent, the borylated products were subjected to Pd-catalyzed cross-coupling reactions. The method was further extended to the synthesis of 2-hydride indole and 2-silyl indoles (2-SiMe2Ph) by using appropriate reagents (HBpin and pinB-SiMe2Ph, respectively). The yields from all the above-mentioned reactions range from moderate to excellent. Substrate scope was well studied.
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