4.8 Article

Acid-promoted Cascade Cyclization to Produce Fused-polycyclic Indole Derivatives

Journal

ORGANIC LETTERS
Volume 15, Issue 12, Pages 2978-2981

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ol401128h

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Funding

  1. Ministry of Education, Culture, Sports, Science, and Technology, Japan
  2. Research Foundation for Pharmaceutical Sciences
  3. JSPS Research Fellowship
  4. Uehara Memorial Foundation
  5. Grants-in-Aid for Scientific Research [23390003] Funding Source: KAKEN

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An acid-promoted novel cascade cyclization is described. Using 8 equiv of trifluoroacetic acid or a catalytic amount of Lewis acid as the promoter, structurally diverse polycyclic cyclopenta[b]indoles were obtained in moderate to excellent yield. This cascade process was extremely effective for the synthesis of 8-membered ring-fused cyclopenta[b]indole derivatives.

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