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Direct radical alkylation and acylation of 2H-indazoles using substituted Hantzsch esters as radical reservoirs

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A platform approach for the direct synthesis of 3-substituted 2H-indazole derivatives has been developed using a Ag(I)/Na2S2O8 system. This regioselective alkylation/acylation protocol operates under mild conditions, tolerates a wide range… Click to show full abstract

A platform approach for the direct synthesis of 3-substituted 2H-indazole derivatives has been developed using a Ag(I)/Na2S2O8 system. This regioselective alkylation/acylation protocol operates under mild conditions, tolerates a wide range of structural moieties and delivers versatile 2H-indazole derivatives with high efficiency. The gram-scale reaction and the application to the synthesis of bioactive molecules further demonstrate the utility of our protocol.

Keywords: radical alkylation; acylation indazoles; alkylation acylation; direct radical; alkylation

Journal Title: Organic chemistry frontiers
Year Published: 2020

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