4.8 Article

Molecular Oxygen-Mediated Minisci-Type Radical Alkylation of Heteroarenes with Boronic Acids

Journal

ORGANIC LETTERS
Volume 19, Issue 24, Pages 6594-6597

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.7b03297

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Funding

  1. National Natural Science Foundation of China [21672089, 21472080]
  2. Natural Science Foundation of the Jiangsu Higher Education Institutions of China [17KJA350001]

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The carbon carbon bond formation via autoxidation of organoboronic acid using 1 atm of O-2 is achieved in a simple, clean, and green fashion. The approach allows a technically facile and environmentally benign access to structurally diverse heteroaromatics with medicinally privileged scaffolds. The strategy also displays its practicality and sustainability in the resynthesis of marketed drugs Crestor and pyrimethamine.

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