广谱抗病毒药物西多福韦的合成  

Practical Synthesis of Cidofovir A Broad-Spectrum Antiviral Drug

作　　者：蒋兴凯[1] 何小羊[1] 郭焕芳[1] 刘琨[1] 马建洲[1] 谢蓝[1] 

机构地区：[1]军事医学科学院毒物药物研究所,北京100850

出　　处：《解放军药学学报》2009年第5期395-397,共3页Pharmaceutical Journal of Chinese People's Liberation Army

摘　　要：目的优化西多福韦的合成工艺。方法利用三苯甲基保护的(R)-缩水甘油经碳酸铯催化与胞嘧啶缩合,二甲基乙缩醛保护氨基后,在NaH作用下引入甲基磷酸二乙酯,再脱去不同的保护基得到西多福韦。结果西多福韦结构经光谱确定;纯度>99.5%,总收率为23%。结论该合成路线短,条件温和,纯化方便,试剂成本低,适合规模化合成制备。Aim To explore a practical scale-up synthesis of cidofovir in labs. Methods Cidofovir was synthesized by condensation between cytosine and protected （ R ）-glyeidol in the presence of Cs2CO3 by protection of amino group protected by dimethylacetal, by esterification with diethyl p-benzen-sulfonyloxymethyl phosphorate in the presence of Nail and by deprotections successively. Results A total yield of 23% was achieved;the purity exceeded 99.5%. The structure was identified by spectrum. Conlusion This synthetic process is suitable for industrial preparation under mild reaction conditions, operation-friendly and cost-effective.

关 键 词：西多福韦 合成 无环核苷 抗病毒药物 

分 类 号：R94[医药卫生—药剂学]