Easily Accessible Benzamide‐Derived P,O Ligands (Bphos) for Palladium‐Catalyzed Carbon–Nitrogen Bond‐Forming Reactions |
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| Authors: | Guoshu Chen Dr. Wai Har Lam Dr. Wai Shan Fok Hang Wai Lee Fuk Yee Kwong Dr. |
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| Affiliation: | 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 |
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| 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. |
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| Keywords: | amination benzamide catalysis palladium phosphines |
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