3.8 Article

Efficient and Convenient Synthesis of Indazol-3(2H)-ones and 2-Aminobenzonitriles

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JOURNAL OF COMBINATORIAL CHEMISTRY
卷 11, 期 6, 页码 1073-1077

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AMER CHEMICAL SOC
DOI: 10.1021/cc9001058

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  1. Foundation of Key Laboratory of Organic Synthesis of Jiangsu Province

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A mild, efficient, one-pot protocol for the synthesis of indazole-3(2H)-ones via cyclization of nitro-aryl substrates through low-valent titanium reagent has been described. The method used Triethylamine (TEA) to control pH. Particularly, 2-aminobenzonitriles were synthesized by one step easily. The mechanistic course of the reaction suggests the involvement of an anion leading to an intramolecular cyclization via N-N bond formation.

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