西多夫韦的合成工艺改进  

Improved synthesis of cidofovir

作　　者：刘剑峰[1] 张瑞环[2] 徐文方[1] 

机构地区：[1]山东大学药学院 [2]济南市中心医院药学部,山东济南250013

出　　处：《中国药物化学杂志》2007年第1期41-43,46,共4页Chinese Journal of Medicinal Chemistry

摘　　要：目的改进核苷类抗病毒药物西多夫韦的合成工艺。方法以(S)-2,3-缩异丙叉甘油醛为起始原料,经还原、酰化、缩合、水解、醚化、酯交换、脱三苯甲基保护、水解、脱苯甲酰基保护、酸化等反应制得抗病毒药物西多夫韦。结果与结论目标化合物结构经1H-NMR、质谱、13C-NMR、红外光谱确证。总收率为7.36%,比文献收率提高了1.56%。改进后的方法反应条件温和、操作简便,有利于工业化生产。Aim To improve the synthetic procedure of cidofovir. Methods Cidofovir was synthesized from （S）-2, 3-O-isopropylglyceraldehyde via reduction, acylation, consendation, hydrolysis, etherification, ester exchange, hydrolysis, deprotection of trityl, deprotection of benzoyl, acidification, etc. Results and conclusion The structure of target compound was confirmed by 1H-NMR, MS, ^13C-NMR, IR, and the overall yield was 7.36 %. Compared with the reported method, the overall yield was improved by 1.56 %. This synthetic process is suitable for industrial preparation by its convenient operation and mild reaction conditions.

关 键 词：西多夫韦 抗病毒药物 (S)-2 3-缩异丙叉甘油醛 

分 类 号：TQ463.5[化学工程—制药化工]