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Easily Accessible Benzamide‐Derived P,O Ligands (Bphos) for Palladium‐Catalyzed Carbon–Nitrogen Bond‐Forming Reactions
Authors:Guoshu Chen Dr  Wai Har Lam Dr  Wai Shan Fok  Hang Wai Lee  Fuk Yee Kwong Dr
Institution:1. State Key Laboratory of Chinese Medicine and Molecular Pharmacology, Shenzhen, China;2. Open Laboratory of Chirotechnology of the Institute of Molecular Technology for Drug Discovery and Synthesis, Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hung Hom, Kowloon, Hong Kong, China, Fax: (+852)?236‐49‐932
Abstract:Easily accessible benzamide‐derived hemilabile phosphine ligands were efficiently prepared through ortho‐directed lithiation of the corresponding N,N‐diethylbenzamide followed by quenching with chlorodialkylphosphines. These structurally simple hemilabile ligands were found to be highly effective in palladium‐catalyzed amination of aryl and heteroaryl chlorides. Various sterically congested and functionalized aryl halide substrates were compatible in these reaction conditions. By using optimized reaction conditions, remarkable catalyst productivity (total turnover number up to 8400) was obtained.
Keywords:amination  benzamide  catalysis  palladium  phosphines
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