N-琥珀酰亚胺-4-^(18)F(氟甲基)苯甲酸酯的合成  

SYNTHESIS OF N-SUCCINIMIDYL-4-^(18) F(FLUOROMETHYL)BENZOATE

作　　者：李俊玲[1] 张秀利[1] 田海滨[1] 周伟[1] 林英武[1] 尹端沚[1] 汪勇先[1] 

机构地区：[1]中国科学院上海原子核研究所,上海201800

出　　处：《核化学与放射化学》2002年第3期157-160,共4页Journal of Nuclear and Radiochemistry

基　　金：国家自然科学基金资助项目 (10 0 75 0 73 );中国科学院创新工程前沿资助项目 (90 2 0 0 15 4)

摘　　要：合成了18F标记蛋白常用中间体N 琥珀酰亚胺 4 18F(氟甲基 )苯甲酸酯 (18F SFMB) ,用操作简单的Sep Pak硅胶柱代替了繁琐耗时的HPLC分离。探讨了反应溶剂、温度、K/ 2 2 2与K2 CO3 的摩尔比及反应时间等诸因素对18F SFMB放化合成的影响。得出较佳标记条件 :以无水乙腈为溶剂 ,K/ 2 2 2与K2 CO3 摩尔比为1,80℃下反应 5min ,标记率为 5 7% ,比文献值提高了 3倍以上。对IgG进行了标记 ,在室温下反应 15min ,标记率可达 88%。N succinimidyl 4 18 F (fluoromethyl)benzoate ( 18 F SFMB) of labeling proteins has been synthesized. Laborious and time consuming HPLC is substituted by simple Sep pak silica during the process of isolation. Many factors affecting the radiochemical synthesis of 18 F SFMB including reaction solvents, temperature, the mole ratio of K/222 to K 2CO 3 and reaction time are studied. The better labeling conditions are as follows:dry acetonitrile as solvent, the mole ratio of K/222 to K 2CO 3 is 1∶1, reaction time is 5 min at 80 ℃. The radiochemical yield is about 57%(EOS) which is about 3 times higher than the published data. IgG is indirectly labeled by 18 F SFMB and the labeled yield are about 88% at room temperature.

关 键 词：合成 N-珀酰亚胺-4-^18F(氟甲基)苯甲酸酯 ^18F-SFMB IgG 氟18 放射性药物 标记 

分 类 号：R817.9[医药卫生—影像医学与核医学]