4.8 Article

Rhodium-Catalyzed Site-Selective Coupling of Indoles with Diazo Esters: C4-Alkylation versus C2-Annulation

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ORGANIC LETTERS
卷 19, 期 22, 页码 6184-6187

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AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.7b03099

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资金

  1. NSFC [21472186, 21525208]
  2. fund for new technology of methanol conversion of Dalian Institute of Chemical Physics (Chinese Academy of Sciences)
  3. Strategic Priority Program of the CAS [XDB17020300]

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A Rh(III)-catalyzed site-selective C-H activation of C(3)-functionalized indoles in a coupling with diazo esters has been realized with carbonyl as a weakly coordinating group. The coupling selectivity is dictated by the temperature and additives, affording either C4-alkylated indoles or C2-annulated lactones in moderate to excellent efficiency.

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