阿德福韦前药的设计与合成  

Design and Synthesis of Adefovir's Prodrug

作　　者：余永游[1] 胡继伟[1] 李勤耕[1] 

机构地区：[1]重庆医科大学药学院,重庆市渝中区医学院路1号400016

出　　处：《光谱实验室》2013年第4期1929-1931,共3页Chinese Journal of Spectroscopy Laboratory

摘　　要：以阿德福韦作起始原料,经氨基保护、卤化而制得磷酰氯,再与1,3-丙二醇类配体缩合成六元环、脱保护制得其肝靶向前药的醋酸盐1a-c,其中1c氢解即可得到1d,总收率为50%—60%。目标化合物的结构经IR、1H NMR、MS确证。The acetate salts of liver targeting prodrug （la-c）, which are regarded adefovir as starting material, have been obtained by amino protection, alogenation, condensation with 1, 3- propylene glycol analogues,followed by deproteetion with an overall yiled of 50%-60%. Then ld is obtained by the hydrogenolysis of lc with the yield of 95%. The structures of target compounds were characterized by IR,1H NMR and MS.

关 键 词：阿德福韦 前药 1 3丙-二醇 合成 

分 类 号：R914.5[医药卫生—药物化学] O657.61[医药卫生—药学]