ONE-STEP SYNTHESIS OF F-18 LABELED [F-18] N-SUCCINIMIDYL 4-(FLUOROMETHYL)BENZOATE FOR PROTEIN LABELING

被引:82
作者
LANG, LX
ECKELMAN, WC
机构
[1] Positron Emission Tomography Department, National Institutes of Health, Bethesda, MD 20892
关键词
D O I
10.1016/0969-8043(94)90031-0
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
[F-18]-N-succinimidyl 4-(fluoromethyl)benzoate (1) has been prepared from N-succinimidyl-4-[(4-nitrobenzensulfonyl)oxymethyl]benzoate (2) in one step using Kryptofix 2.2.2/[F-18(-)]. The effect of solvents, potassium salts and temperatures were studied to determine optimum labeling condition. The best results were obtained using carbonate as the counter ion and acetone as the solvent at room temperature. Overall radiochemical yields of similar to 18% (EOS) for the synthesis of 1 were obtained in 30-35 min, including HPLC purification. Proteins were labeled with 1 with labeling yields of 50-70% in 15 min.
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页码:1155 / 1163
页数:9
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