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Copper catalyzed tandem Chan–Lam type C—N and Staudinger-phosphite N—P coupling for the synthesis of N-arylphosphoramidates
Catalysis Communications ( IF 3.7 ) Pub Date : 2018-10-09 , DOI: 10.1016/j.catcom.2018.10.006
Nisar A. Dangroo , Tabassum Ara , Bashir A. Dar , M.A. Khuroo

A copper(II)-catalyzed one-pot conversion of aryl/heteroaryl boronic acids to N-aryl phosphoramidates via a tandem Chan–Lam and Staudinger-phosphite coupling has been reported. The method is highly efficient, economical and safe involving in-situ generation of organic azides. The method was successfully extended to boronic esters and potassium organotrifluoroborate salts, however, the organoboranes with B–C(sp3) were found to be unreactive under the reaction conditions. The current method has a wide substrates scope and offers the possibility of synthesizing phosphoramidates in good yield, and notably, the mild reaction conditions used allow for potentially sensitive functionalities to be used in the developed protocol are of great importance in drug discovery.



中文翻译:

铜催化串联的Chan-Lam CN型和Staudinger-亚磷酸酯N-P偶联,用于合成N-芳基磷酰胺

据报道,通过串联的Chan-Lam和Staudinger-亚磷酸酯偶联反应,铜(II)催化一锅法将芳基/杂芳基硼酸转变为N-芳基氨基磷酸酯。该方法是高效,经济和安全的,涉及就地生成有机叠氮化物。该方法已成功地扩展到硼酸酯和有机三氟硼酸钾盐,但是,带有B–C(sp 3的有机硼烷被发现在反应条件下是不反应的。当前的方法具有广泛的底物范围,并提供了以高收率合成氨基磷酸酯的可能性,并且值得注意的是,所用的温和反应条件允许在开发的方案中使用潜在的敏感功能在药物开发中非常重要。

更新日期:2018-10-09
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