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June 17, 2026Advanced Synthesis & Catalysis

Chemoselective Synthesis of 2,2‐Disubstituted Indolin‐3‐Ones via Palladium‐Catalyzed Allylation of 3‐Hydroxyindoles

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Authors

CYChi YangUniversity of Science and Technology of ChinaQZQi ZhangJinan UniversityLGLeyang GuanChina Pharmaceutical University

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Overview

Randomized trial demonstrates efficient synthesis of indolin-3-ones in organic chemistry, suggesting new methods for diverse transformations.

Key Points

  • The aim is to develop efficient methods for synthesizing 2,2-disubstituted indolin-3-ones, which are significant in both structural and biological contexts.
  • Utilized palladium-catalyzed allylation of 3-hydroxyindoles with internal alkynes and gem-difluorocyclopropanes.
  • Employed redox-neutral conditions for direct synthesis of 2-allyl-2-carboxylate-indolin-3-ones.
  • Demonstrated broad substrate scope and excellent functional group tolerance.
  • Successfully synthesized 2-allyl-2-carboxylate-indolin-3-ones under mild conditions with high yield.
  • Achieved introduction of fluorine atoms and construction of C2 all-carbon quaternary center in a single step.
  • Facilitated rapid access to complex biologically relevant heterocycles through downstream transformations.

Cite This Study

Yang et al. (2026) studied this question.

synapsesocial.com/papers/6a323bbcd50b63ecad206432https://doi.org/10.1002/adsc.70587
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