2'-脱氧胞苷的合成工艺

来源 :精细化工 | 被引量 : 0次 | 上传用户:zhenzhurujun
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以α-D-2-脱氧核糖和尿嘧啶为起始原料,经过甲苷化、酯化、氯代、亲核取代、高效氨化及水解脱保护6个步骤,经一次重结晶,以43.6%的总收率得到β-D-2’-脱氧胞苷,纯化后HPLC纯度达99%。产物结构经1HNMR、HPLC表征。目前已经实现公斤级别的生产。 Α-D-2-deoxyribose and uracil as starting materials, after six steps of glycosidation, esterification, chlorination, nucleophilic substitution, efficient ammoniation and hydrolysis deprotection, after a recrystallization to 43.6 The total yield of β-D-2’-deoxycytidine was obtained in% yield and the HPLC purity was 99% after purification. The product structure was characterized by 1HNMR, HPLC. Kilo-class production has now been achieved.
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