Abstract

A simple, efficient, and novel method is developed for the synthesis of phosphoroamidates via an Atherton–Todd coupling reaction of amines with dialkyl H-phosphite using trichloroisocyanuric acid as an efficient and safe reagent. Treatment of amines with dialkyl H-phosphite and trichloroisocyanuric acid under base-free conditions gives phosphoroamidates in moderate to good yields. The reaction proceeded effectively to afford the corresponding phosphoroamidates via a dehydrogenative coupling of H-phosphonates with amines. This method is easy, rapid, and good-yielding for the synthesis of phosphoroamidates.

A simple, efficient, and novel method is developed for the synthesis of phosphoroamidates via an Atherton–Todd coupling reaction of amines with dialkyl H-phosphite using trichloroisocyanuric acid as an efficient and safe reagent. Treatment of amines with dialkyl H-phosphite and trichloroisocyanuric acid under base-free conditions gives phosphoroamidates in moderate to good yields. The reaction proceeded effectively to afford the corresponding phosphoroamidates via a dehydrogenative coupling of H-phosphonates with amines. This method is easy, rapid, and good-yielding for the synthesis of phosphoroamidates.

中文翻译：

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三氯异氰尿酸是在无碱条件下通过Atherton-Todd反应合成磷酰胺的有效试剂

摘要

通过使用三氯异氰尿酸作为有效和安全的试剂，通过胺与亚磷酸二烷基酯的Atherton-Todd偶联反应，开发了一种简单，高效且新颖的方法来合成氨基膦酸酯。在无碱条件下用亚磷酸氢二烷基酯和三氯异氰尿酸处理胺，可得到中等至良好收率的氨基磷酸酯。反应通过H-膦酸酯与胺的脱氢偶联有效地进行，得到相应的氨基磷酸酯。该方法简便，快速且产率高，可用于合成磷酰胺。

通过使用三氯异氰尿酸作为有效和安全的试剂，通过胺与亚磷酸二烷基酯的Atherton-Todd偶联反应，开发了一种简单，高效且新颖的方法来合成氨基膦酸酯。在无碱条件下用亚磷酸氢二烷基酯和三氯异氰尿酸处理胺，可得到中等至良好收率的氨基磷酸酯。反应通过H-膦酸酯与胺的脱氢偶联有效地进行，得到相应的氨基磷酸酯。该方法简便，快速且产率高，可用于合成磷酰胺。