Journal
ADVANCED SYNTHESIS & CATALYSIS
Volume 362, Issue 23, Pages 5170-5195Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/adsc.202000930
Keywords
Indole derivatives; propargylic alcohols; tandem annulations; cyclization reactions; acid catalysis
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Funding
- National Natural Science Foundation of China [21801027]
- Open Project Program of Antibiotics Research and Re-evaluation Key Laboratory of Sichuan Province [ARRLKF19-07]
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Indole derivatives are important heterocycles in organic synthesis for serving as privileged building blocks for functional material and as key components in a lot of bioactive compounds. Propargylic alcohols, bearing alkynyl and hydroxyl functional groups, have emerged as promising feedstock materials for the construction of carbo- and heterocycles. Especially, in the last decade, the Lewis or Bronsted acid catalysed tandem annulations of propargylic alcohols to build structurally diverse indole derivatives have been well-investigated. In this review, we summarize two main synthetic strategies toward indole derivatives via the cascade reactions of propargylic alcohols: indole-ring formation involved tandem reactions and the direct function-alization of indole skeletons. We hope this review would help to develop new and more efficient protocols for the synthesis of indole-included N-heterocycles.
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