4.7 Article

Efficient synthesis of 2-substituted azoles: radical C-H alkylation of azoles with dicumyl peroxide, methylarenes and cycloalkanes under metal-free condition

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ORGANIC CHEMISTRY FRONTIERS
卷 4, 期 10, 页码 2039-2043

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ROYAL SOC CHEMISTRY
DOI: 10.1039/c7qo00396j

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资金

  1. Natural Science Foundation of Jiangsu Province [BK 20131346, BK 20140776]
  2. National Natural Science Foundation of China [21476116, 21402093]
  3. Chinese Postdoctoral Science Foundation [2015M571761, 2016T90465]

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A simple and efficient synthesis of 2-substituted azoles by alkylation of azoles with dicumyl peroxide, methylarenes and cycloalkanes under metal-free condition has been developed. The transformation can proceed smoothly in the presence of tert-butyl peroxide (DTBP) as an oxidant and dicumyl peroxide (DCP) as a methylation reagent with wide substrate scope and good yields. Mechanistic details including radical reaction process are also described.

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