作者:Guillaume Laconde、Muriel Amblard、Jean Martinez
DOI:10.1016/j.tetlet.2018.12.046
日期:2019.1
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
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。