【摘要】 以4-溴苯酚、溴代正戊烷为起始原料,经加成、硼代、偶联、水解、酯化共5步反应得到阿尼芬净侧链,其结构经过¹H-NHR、MS等分析测试技术进行确认。得出的最佳合成工艺:以硼代产物为原料、Pd（dppf）Cl₂为催化剂来进行偶联反应,得到的对戊氧基三联苯甲酸（Ⅳ）与羟基苯并三唑反应制备目标产物活性酯。该合成阿尼芬净侧链工艺总收率达到50.8%。更多还原

【Abstract】 Taking 4-bromophenol and bromo-n-pentane as starting materials, anidulafungin side chain was obtained through five steps of addition, boron generation, coupling, hydrolysis and esterification, which structure was confirmed by ¹ H-NHR, MS and other analytical testing techniques. The obtained optimum synthesis process is the active esters is prepared by coupling reaction of P-pentoxytribenzoic acid Ⅳ with hydroxybenzotriazole using boron product as raw material and Pd（dppf）Cl₂ as catalyst. The total yield of the synthesis process of anidulafungin side chain reachs 50.8%.更多还原