A Cascade Phosphinoylation/Cyclization/Desulfonylation Process for the Synthesis of 3-Phosphinoylindoles

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• 作者：Yuzhen Gao ; Guozhang Lu ; Pengbo Zhang ; Liangliang Zhang ; Guo Tang ; Yufen Zhao
• 刊名：Organic Letters
• 出版年：2016
• 出版时间：March 18, 2016
• 年：2016
• 卷：18
• 期：6
• 页码：1242-1245
• 全文大小：368K
• ISSN：1523-7052

文摘

3-Phosphinoylindole derivatives play important roles as pharmaceutical drugs and ligands. A new method for the synthesis of 3-phosphinoylindole derivatives has been achieved through silver-mediated cycloaddition between N-Ts-2-alkynylaniline derivatives and H-phosphine oxides. This transformation offers a straightforward route to the formation of the C–P bond, indole ring, and desulfonylation in one step.