2'-脱氧胞苷的合成工艺

Synthetic Process of 2'-Deoxycytidine

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。

A synthetic process to manufacture 2＇- Deoxycytidine was reported. This process was carried out using α-D-2-Deoxyribose and uracil as economical starting materials after six reaction steps, including a methyl-glycosidation, esterification, chlorination, nucleophilic substitution, efficient amination and hydrolysis deprotection reaction. 2＇-Deoxycytidine obtained an overall yield of 43.6% and a purity of higher than 99% by HPLC after recrystallization. The structure of final product was determined by 1HNMR and HPLC, 2＇-Deoxycytidine has completed a kilogram - scale manufacture in the chemical factory.