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

    • 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.

       

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