Palladium-catalyzed cyclization of o-alkynyltrifluoroacetanilides followed by isocyanide insertion: synthesis of 2-substituted 1H-indole-3-carboxamides |
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| Authors: | Hu Ziwei Liang Dongdong Zhao Jiaji Huang Jinbo Zhu Qiang |
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| Affiliation: | State Key Laboratory of Respiratory Disease, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, 190 Kaiyuan Avenue, Guangzhou 510530, China. |
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| Abstract: | A base-controlled synthesis of 2-substituted secondary and tertiary 1H-indole-3-carboxamides through PdCl(2)-catalyzed cyclization of o-alkynyltrifluoroacetanilides followed by isocyanide insertion has been developed. The reaction proceeds smoothly at ambient temperature using O(2) in air as the sole oxidant of the palladium catalyst. |
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