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Synthesis of 1H-Indazoles via Silver(I)-Mediated Intramolecular Oxidative C-H Bond Amination.


ABSTRACT: We described a silver(I)-mediated intramolecular oxidative C-H amination that enables the construction of assorted 1H-indazoles that are widely applicable in medicinal chemistry. The developed amination was found to be efficient for the synthesis of a variety of 3-substituted indazoles that are otherwise difficult to be synthesized by other means of C-H aminations. Preliminary mechanistic studies suggested that the current amination proceeds via single electron transfer (SET) mediated by Ag(I) oxidant.

SUBMITTER: Park A 

PROVIDER: S-EPMC7948442 | biostudies-literature | 2021 Mar

REPOSITORIES: biostudies-literature

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Synthesis of 1<i>H</i>-Indazoles via Silver(I)-Mediated Intramolecular Oxidative C-H Bond Amination.

Park Areum A   Jeong Kyu-Sung KS   Lee Hyuk H   Kim Hyunwoo H  

ACS omega 20210223 9


We described a silver(I)-mediated intramolecular oxidative C-H amination that enables the construction of assorted 1<i>H</i>-indazoles that are widely applicable in medicinal chemistry. The developed amination was found to be efficient for the synthesis of a variety of 3-substituted indazoles that are otherwise difficult to be synthesized by other means of C-H aminations. Preliminary mechanistic studies suggested that the current amination proceeds via single electron transfer (SET) mediated by  ...[more]

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