4.7 Article

Multidirectional Synthesis of Substituted Indazoles via Iridium-Catalyzed C-H Borylation

Journal

JOURNAL OF ORGANIC CHEMISTRY
Volume 80, Issue 10, Pages 5308-5314

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.5b00452

Keywords

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Funding

  1. EPSRC
  2. Pfizer Neusentis
  3. Astra Zeneca
  4. Engineering and Physical Sciences Research Council [1354666, EP/F068158/1, 1355114] Funding Source: researchfish
  5. EPSRC [EP/F068158/1] Funding Source: UKRI

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In the absence of a steric directing group, iridium-catalyzed. C-H borylation of N-protected indazoles occurs rapidly and selectively at C-3 and the resulting boronate esters can be utilized in a range of downstream conversions. The functional group tolerance of the iridium-catalyzed C-H borylation reaction enables simple and efficient multidirectional syntheses of substituted indazoles to be realized.

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