4.8 Article

Selective Synthesis of Pyrazolo[1,2-a]pyrazolones and 2-Acylindoles via Rh(III)-Catalyzed Tunable Redox-Neutral Coupling of 1-Phenylpyrazolidinones with Alkynyl Cyclobutanols

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ORGANIC LETTERS
卷 22, 期 12, 页码 4697-4702

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AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.0c01475

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资金

  1. National Natural Science Foundation of China (NSFC) [21572047]
  2. Program for Innovative Research Team in Science and Technology in Universities of Henan Province [20IRTSTHN005]
  3. Key Project of Science and Technology of Henan Province [192102310412]
  4. 111 Project [D17007]

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An unprecedented divergent synthesis of pyrazolo[1,2-a]pyrazolones and 2-acylindoles via Rh(III)-catalyzed [4 + 1] or [3 + 2] annulation of 1-phenylpyrazolidinones with alkynyl cyclobutanols through redox-neutral multiple bond activation by using -NH and -OH units as directing groups is presented. Notably, different annulation reactions were selectively achieved by simply adjusting the reaction conditions. With features such as simple procedures, easily accessible substrates, and high regio/chemoselectivity, these methods may find wide applications in related areas.

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