含羧基的偕二膦酸酯的合成  

The Synthesis of Gem-Bisphosphonates with Carboxylic Group

作　　者：郭子维[1] 郭丽[1] 李佩杰[1] 吴勇[1] 

机构地区：[1]四川大学华西药学院,成都610041

出　　处：《四川大学学报（自然科学版）》2002年第5期922-924,共3页Journal of Sichuan University(Natural Science Edition)

基　　金：国家自然科学基金 (39970 86 9)

摘　　要：作者以二苄胺 (2 )、原甲酸三乙酯以及亚磷酸二乙酯 (3)为原料经四步反应合成了含羧基的偕二膦酸酯 (1) ,总收率 4 4 %～ 4 5 % .目标物结构经IR ,1HNMR和元素分析确证 .结果表明 ,该方法实验操作简单 ,收率高 ,该反应是合成含羧基的偕二膦酸酯 (1)The synthetic method of gem-bisphosphonate with carboxylic group was studied. The gem-bisphosphonates with carboxylic group (1a～1c) were synthesized via four steps with 42%～45% overall yield starting from dibenzyl amino (2) , triethyl orthoformate and diethyl phosphite(3). The structure of compounds (1a～1c) were comfirmed by IR, 1HNMR and elemental analysis. Result demonstrates that the method of synthesis of compounds (1a～1c) is an effective method.

关 键 词：羧基 偕二膦酸酯 合成 骨靶向性载体 骨靶向药物 二苄胺 原甲酸三乙酯 亚磷酸二乙酯 

分 类 号：R914.5[医药卫生—药物化学]