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Access to 2-Substitued-2H-Indazoles via Copper-Catalyzed Regioselective Cross-Coupling Reaction

Abstract

A CuCl catalyzed C-N cross-coupling reaction using commercially available 1H-indazoles with diaryliodonium salts is described. The methodology features ample structural versatility, affording 2-substituted-2H-indazole in good yields and complete N(2)-regiocontrol. Furthermore, the utility of the reaction was demonstrated in the synthesis of the known estrogen receptor β agonist. Mechanistic studies by density functional theory calculations suggested that the complete regioselectivity can be attributed that the only weak base TfO- in our system could not deprotonate indazoles, and the catalyst oxidation process would be the rate-determining step.

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Publication details

The article was received on 16 Jan 2018, accepted on 15 Feb 2018 and first published on 15 Feb 2018


Article type: Communication
DOI: 10.1039/C8OB00128F
Citation: Org. Biomol. Chem., 2018, Accepted Manuscript
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    Access to 2-Substitued-2H-Indazoles via Copper-Catalyzed Regioselective Cross-Coupling Reaction

    R. Zhang , Z. Liu, Q. Peng, Y. Zhou, L. xu and X. Pan, Org. Biomol. Chem., 2018, Accepted Manuscript , DOI: 10.1039/C8OB00128F

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