Selective amination of polyhalopyridines catalyzed by a palladium-xantphos complex |
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Authors: | Ji Jianguo Li Tao Bunnelle William H |
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Institution: | Neuroscience Research, Global Pharmaceutical Research and Development, Department-R47W, AP9A-1, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064, USA. jianguo.ji@abbott.com |
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Abstract: | reaction: see text] Amination of 5-bromo-2-chloropyridine (1a) catalyzed by a palladium-Xantphos complex predominately gives 5-amino-2-chloropyridine product 3a in 96% isolated yield and excellent chemoselectivity (3a/4a = 97:3). Amination of 2,5-dibromopyridine (11) under the same conditions exclusively affords 2-amino-5-bromopyridine 4a. |
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