脂糖肽抗生素Telavancin的合成工艺改进

Process Improvement on the Synthesis of Lipoglycopeptide Antibiotic Telavancin

以万古霉素盐酸盐为原料,与N-Fmoc-癸基氨基乙醛生成席夫碱后再经还原、脱Fmoc保护、与氨甲基膦酸进行曼尼希反应合成了Telavancin,总收率36.3%,其结构经1H NMR和MS确证。

Telavancin in total yield of 36.3% was synthesized from vancomycin hydrochloride by the reaction with N-Fmoc-decyl-aminoacetaldehyd,followed by reductive amination,deprotection and then Mannich reacted with aminomethylphosphonic acid.The structure was confirmed by 1H NMR and MS.