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Ligand‐Promoted Borylation of C(sp3)H Bonds with Palladium(II) Catalysts
Authors:Jian He  Heng Jiang  Ryosuke Takise  Ru‐Yi Zhu  Dr Gang Chen  Prof?Dr Hui‐Xiong Dai  Dr T G Murali Dhar  Dr Jun Shi  Dr Hao Zhang  Dr Peter T W Cheng  Prof?Dr Jin‐Quan Yu
Institution:1. Department of Chemistry, The Scripps Research Institute (TSRI), 10550 North Torrey Pines Road, La Jolla, CA 92037 (USA);2. Discovery Chemistry, Bristol‐Myers Squibb Company, Route 206 and Provinceline Road, Princeton, NJ 08543 (USA);3. Discovery Chemistry, Bristol‐Myers Squibb Company, 311 Pennington Rocky Hill Road, Pennington, NJ 08534 (USA)
Abstract:A quinoline‐based ligand effectively promotes the palladium‐catalyzed borylation of C(sp3)? H bonds. Primary β‐C(sp3)? H bonds in carboxylic acid derivatives as well as secondary C(sp3)? H bonds in a variety of carbocyclic rings, including cyclopropanes, cyclobutanes, cyclopentanes, cyclohexanes, and cycloheptanes, can thus be borylated. This directed borylation method complements existing iridium(I)‐ and rhodium(I)‐catalyzed C? H borylation reactions in terms of scope and operational conditions.
Keywords:amino acids  borylation  C  H activation  palladium  synthetic methods
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