Affiliation:
1. Inner Mongolia Key Laboratory of Fine Organic Synthesis College of Chemistry and Chemical Engineering Inner Mongolia University 235 Daxue West Rd Hohhot 010021 People's Republic of China
Abstract
AbstractCu‐catalyzed intramolecular borylation‐cross coupling reaction of alkenes was developed. Racemic and chiral borylated indolines were achieved by borylation‐cross coupling 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‐substituted borylated indoline was obtained in 80% yield and 80:20 er with (R, R)‐Me‐Duphos. Application of 3‐substituted borylated indolines has been demonstrated by a gram scale synthesis and further functionalization.
Funder
National Natural Science Foundation of China
Natural Science Foundation of Inner Mongolia Autonomous Region
Inner Mongolia University