万古霉素衍生物——特拉万星的合成方法改进

Process Improvement on the Synthesis of Telavancin-Derivative of Vancomycin

将特拉万星的合成路线进行了工艺改进,通过连续反应方法制得关键中间体N-Fmoc-癸基氨基乙醛,然后经一锅法及曼尼希反应,反相硅胶制备得到特拉万星盐酸盐.HPLC纯度及收率均高于已有文献报道,且整条路线操作简便,成本更低,环境友好,适于工业化生产.

This article was the process improvement of telavancin synthesis. The key intermediate N-Fmoc-decyl-aminoacetaldehyde was obtained through continuous reaction method, followed by one-pot condensation and Mannich reaction. Telavancin hydrochloride was finnally obtained via reversed phase silica gel. The HPLC purity and total yield of this route were higher than the existing literatures. It was easy to operate, environmentally friendly, lower costs, and suitable for industrialized production.