2'-脱氧核糖胞苷的合成工艺
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TQ223

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Process Development of 2'-Deoxycytidine
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    摘要:

    本文报道了2'-脱氧核糖胞苷的一条工业化生产的路线。该工艺路线以α-D-2-脱氧核糖和尿嘧啶为原料,经过甲苷化,酯化,氯代,亲核取代,高效氨化及水解脱保护等6个步骤,总收率44%,经一次重结晶纯化最终产品纯度达到99%以上。此路线条件温和,操作安全,终产物分离纯化简易。目前已经完成公斤级别的中试。

    Abstract:

    Herein, we reported an efficient method to manufacture 2'-Deoxycytidine. This process, which is using α-D-2-Deoxyribose and Uracil as economical starting material, went through 6 linear steps, including methyl-glycosidation, protection, chlorination, nucleophilic substitution, amination and deprotection reactions. The final product is obtained as 44% overall yield and 99% purity after recrystallization. This process has several advantages, such as mild reaction conditions, relative safe operation and straightforward purification for final product and intermediates. Up to now, kg-scale manufacture of 2-Deoxycytidine is completed in the chemical factory.

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李江南,李金岭,李明,姜申德.2'-脱氧核糖胞苷的合成工艺[J].精细化工,2016,33(9):

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  • 收稿日期:2016-03-18
  • 最后修改日期:2016-05-14
  • 录用日期:2016-05-23
  • 在线发布日期: 2016-08-17
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