4.7 Article

A Straightforward Approach to Fluorinated Pyrimido[1,2-b]indazole Derivatives via Metal/Additive-Free Annulation with Enaminones, 3-Aminoindazoles, and Selectfluor

Journal

JOURNAL OF ORGANIC CHEMISTRY
Volume 87, Issue 10, Pages 6562-6572

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.2c00136

Keywords

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Funding

  1. National Natural Science Foundation of China [22071171]
  2. Natural Science Foundation of Zhejiang Province [LZ22B020003]

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A novel and efficient three-component reaction for the synthesis of fluorinated pyrimido[1,2-b]indazole derivatives is reported. This transformation shows excellent functional group compatibility, without the need for metal catalysts or additives. It holds great significance for the synthesis and application of fluorinated heterocycles.
A novel and efficient three-component reaction with two C-N bonds and one C-F bond formation has beenreported, which provides a straightforward route to a variety offluorinated pyrimido[1,2-b]indazole derivatives. This transformationhas the advantage of excellent functional group compatibility, including aliphatic and aromatic substituents enaminones. Moreover,metal and additives are not necessary for this reaction, which is of great significance for the synthesis and application offluorinatedheterocycles

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