No-carrier-added (4-fluoro-3-[131I]iodobenzyl)guanidine and (3-[211At]astato-4-fluorobenzyl)guanidine.
No-carrier-added (4-fluoro-3-[131I]iodobenzyl)guanidine and (3-[211At]astato-4-fluorobenzyl)guanidine.
复制标题
未添加载体的(4-氟-3-[131I]碘苄基)胍和(3-[211At]阿斯托基-4-氟苄基)胍。
DOI：
10.1021/bc950078i
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发表时间：
1996
期刊：
影响因子：
--
通讯作者：
Zalutsky,MR
中科院分区：
文献类型：
--
作者：
Vaidyanathan,G;Affleck,DJ;Zalutsky,MR
With 3-bromo-4-fluorotoluene as starting material, [4-fluoro-3-(trimethylsilyl)benzyl]guanidine was prepared in five steps in 1.5% overall yield. Radioiodination of this silicon precursor usingN-chlorosuccinimide in trifluoroacetic acid at room temperature for 5 min gave (4-fluoro-3-[131I]iodobenzyl)guanidine ([131I]FIBG) in 50−60% radiochemical yield. A byproduct which had a retention time in two HPLC systems similar to that of (m-iodobenzyl)guanidine (MIBG) was formed in about 30% yield. [131I]FIBG was stable up to 3 h under these conditions of iodination, indicating that the byproduct is not generated as a result of [131I]FIBG degradation. Using hydrogen peroxide as the oxidant in aqueous medium and a reaction time of 30 min at 50 °C, yields of [131I]FIBG could be increased to 75−80%, with less than 7% of the byproduct formed under these conditions. Astatination of the silicon precursor usingN-chlorosuccinimide in trifluoroacetic acid at 70 °C gave 65−70% radiochemical yield of (3-[211At]astato-4-fluorobenzyl)guanidine ([211At]AFBG) in 10−15 min; about 17% of the byproduct formation was seen. Astatination of the silicon precursor under aqueous conditions using hydrogen peroxide was not successful.
