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N-琥珀酰亚胺-4-18F(氟甲基)苯甲酸酯的合成

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

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【作者】 李俊玲张秀利田海滨周伟林英武尹端沚汪勇先

【Author】 LI Jun ling, ZHANG Xiu li, TIAN Hai bin, ZHOU Wei, LIN Ying wu, YIN Duan zhi, WANG Yong xianShanghai Institute of Nuclear Research, the Chinese Academy of Sciences, Shanghai 201800, China

【机构】 中国科学院上海原子核研究所中国科学院上海原子核研究所 上海201800上海201800?

【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%。

【Abstract】 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.

【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)
  • 【文献出处】 核化学与放射化学 ,Journal of Nuclear and Radiochemistry , 编辑部邮箱 ,2002年03期
  • 【分类号】O625
  • 【被引频次】3
  • 【下载频次】69
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