Zhang Ming-Rong, Kumata Katsushi, Takei Makoto, Fukumura Toshimitsu, Suzuki Kazutoshi
Department of Molecular Probes, Molecular Imaging Center, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba 263-8555, Japan.
Appl Radiat Isot. 2008 Oct;66(10):1341-5. doi: 10.1016/j.apradiso.2008.04.011. Epub 2008 Apr 22.
The aim of this study was how to introduce radioactive chlorine (*Cl) isotope into a benzene ring to afford *Cl-labeled chlorobenzene ([*Cl]1). Using tributylphenylstannyl compound (2) as a starting material, we determined two routes for introducing *Cl into the benzene ring: reaction of [*Cl]Cl(-) with 2 in the presence of chloramine-T and nucleophilic reaction of [*Cl]Cl(-) with diphenyliodonium tosylate (3). The two routes provide suitable tools to prepare [*Cl]1 without electron-abstracting group in the benzene ring.
本研究的目的是如何将放射性氯（Cl）同位素引入苯环以得到Cl标记的氯苯（[Cl]1）。以三丁基苯基锡化合物（2）为起始原料，我们确定了两条将Cl引入苯环的路线：[*Cl]Cl(-)与2在氯胺-T存在下的反应以及[*Cl]Cl(-)与对甲苯磺酸二苯基碘鎓（3）的亲核反应。这两条路线为制备苯环上无吸电子基团的[*Cl]1提供了合适的方法。
