4.5 Article

A para-C-H Functionalization of Aniline Derivatives via In situ Generated Bulky Hypervalent Iodinium Reagents

期刊

EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
卷 2018, 期 43, 页码 5972-5979

出版社

WILEY-V C H VERLAG GMBH
DOI: 10.1002/ejoc.201801058

关键词

Iodine-mediated reactions; Arenes; C-H activation; Hypervalent iodinium reagents; Reaction mechanisms; Steric control

资金

  1. National Natural Science Foundation of China [21502046]
  2. Natural Science Foundation of Heilongjiang Province [B2016008]
  3. University Nursing Program for Young Scholars with Creative Talents in Heilongjiang Province [UNPYSCT-2017124]
  4. Fundamental Research Funds for the Central Universities from Harbin Engineering University [HEUCFD1412, HEUCFJ161002, HEUCFJ 171006, HEUCFJ181008]

向作者/读者索取更多资源

A practical para-C-H functionalization of aniline derivatives has been developed using an in situ generated bulky hypervalent iodinium reagent. Para-iodo, bromo, chloro, nitro, trifluormethyl aniline derivatives can be obtained efficiently, in many cases in 10 min in a transition metal-free manner. Medicinal chemicals or intermediates can be purified without column chromatography or recrystallization, which significantly reduces the waste and simplifies the work-up process.

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