【摘要】 为了方便快捷地制备嘧啶核苷-肽缀合物,我们发展了一种一釜合成的方法。从尿嘧啶核苷出发,经过4步制备了关键中间体5-乙酰巯亚甲基-2′,3′-二-O-异亚丙基尿苷(4)。在酸性条件下,脱除化合物4的乙酰基,同时游离的巯基与PySS-R(8,12,15,Py=2-吡啶基,R=氨基酸或肽)反应形成新的二硫键,即形成了尿苷与氨基酸或肽以二硫键连接的缀合物(9,13,2)。更多还原

【Abstract】 In order to prepare pyrimidine nucleoside-peptide conjugate concisely,we developed a one-pot synthetic strategy. Started from uridine,5-S-acetyl-thiomethyl-2’,3’-di-O-isopropylidene-uridine(4)was synthesized as the key intermediate in four steps.Under acidic condition,compound 4 was deprotected and reacted with PySS-R(8,12,15,Py=2-pyridyl,R=amino acid or peptide)in one pot to form uridine conjugates(9,13,2)with disulfide bond as linker.更多还原