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.
               
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