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A simple and versatile method to synthesize N-acyl-benzotriazoles
Tetrahedron Letters ( IF 1.8 ) Pub Date : 2018-12-21 , DOI: 10.1016/j.tetlet.2018.12.046
Guillaume Laconde , Muriel Amblard , Jean Martinez

An efficient method for the synthesis of N-acyl-benzotriazoles from a wide variety of protected amino acids, as well as from compounds frequently used in drug discovery such as biotin and N-Fmoc polyethylene glycol, has been developed. The reaction of carboxylic acid derivatives with benzotriazole in the presence of T3P® yielded the corresponding N-acyl-benzotriazoles, which were obtained in high purity following a simple work-up procedure, in most cases via precipitation of the desired product in water.



中文翻译:

一种简单而通用的合成N-酰基-苯并三唑的方法

已经开发了一种有效的方法,该方法可以从多种受保护的氨基酸以及药物开发中常用的化合物(如生物素和N -Fmoc聚乙二醇)合成N-酰基-苯并三唑。在存在下,羧酸衍生物与苯并三唑的反应产生相应的N-酰基-苯并三唑,其通过简单的后处理程序以高纯度获得,在大多数情况下是通过将所需产物在水中沉淀而获得的。

更新日期:2018-12-21
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