Ca(II)-Catalyzed Cascade Reaction of Tryptamines with Propargylic Alcohols: Temperature-Driven Ring Opening and Closing via the Allene Migration Pathway for the Synthesis of Pyrrolo[1,2‑a]indoles
  • Kale, Ashok
  • Kwon, Su Jeong
  • Lee, Joohan
  • Lee, Jae Kyun
  • Lee, Kyeong
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초록

A temperature-dependent cascade of reactions between tryptamines and propargylic alcohols was developed to achieve selective formation of pyrroloindoline and pyrrolo[1,2-a]indole heterocycles by Ca(II) catalysis. The cascade consists of electrophilic addition of allene at the C3 carbon of indole followed by intramolecular cyclization at 60 degrees C to yield pyrroloindolines. Furthermore, simultaneous 1,2-allene migration and pyrrolidine ring opening were followed by intramolecular cyclization via C-N bond formation at reflux temperature to obtain pyrrolo[1,2-a]indole scaffolds. A wide range of substrates, a clean reaction profile, scalability, and good to excellent yields are the advantages of this protocol.

키워드

CarbonTryptamineAlcohol DerivativeCarbonTryptamineTryptamine DerivativeArticleCatalysisControlled StudyCyclizationDrug AnalysisDrug DevelopmentElectrophilicityRing OpeningSignal TransductionSynthesisTemperatureANTIFUNGAL ACTIVITYCYCLIZATIONALKALOIDS
제목
Ca(II)-Catalyzed Cascade Reaction of Tryptamines with Propargylic Alcohols: Temperature-Driven Ring Opening and Closing via the Allene Migration Pathway for the Synthesis of Pyrrolo[1,2‑a]indoles
저자
Kale, AshokKwon, Su JeongLee, JoohanLee, Jae KyunLee, Kyeong
DOI
10.1021/acs.orglett.3c04357
발행일
2024-02
유형
Article
저널명
Organic Letters
26
6
페이지
1196 ~ 1200