4.8 Article

Metal-Free Ortho C-H Borylation of 2-Phenoxypyridines under Mild Conditions

Journal

ORGANIC LETTERS
Volume 14, Issue 10, Pages 2618-2621

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ol300950r

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Funding

  1. National Natural Science Foundation of China [20972083, 21172128, 21105054]
  2. Ministry of Science and Technology of China [2012CB722600]

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An efficient metal-free ortho C-H borylation has been developed via sequential borylation of substituted 2-phenoxypyridines with BBr3 following esterification with pinacol. The corresponding aryl boronates were obtained in good yields. The synthesized aryl boronates can be easily transformed into various useful products. Therefore, the present method makes functionalizations of aryl C-H bonds easy.

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