Abstract:Efficient Cu-catalyzed intramolecular Heck-borylation of alkenes was developed. Racemic and chiral boronated indolines were achieved by borarylation of alkenes with B2pin2 via simultaneous construction of C-C and C-B bonds by Cu/phosphine ligand system. With CuOAc and DPPE ligand, a series of 3-substituted borylated indoline derivatives were concisely synthesized in good to excellent yields in short time under mild conditions. Asymmetric synthesis was investigated by ligand screening, and the chiral 3-substitu… Show more
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