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用碘 - 125标记的抗病毒剂1 - (2 - 脱氧 - 2 - 氟 - β - D - 阿拉伯呋喃糖基)-5 - 碘胞嘧啶(FIAC)的合成与纯化

Synthesis and purification of the anti-viral agent 1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)-5-iodocytosine (FIAC) labeled with iodine-125.

作者信息

Perlman M E, Conti P S, Schmall B, Watanabe K A

出版信息

Int J Nucl Med Biol. 1984;11(3-4):215-8. doi: 10.1016/0047-0740(84)90002-0.

Abstract

The 125I labeled analog of 1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)-5-iodocytosine (FIAC) has been prepared for studies on the imaging of herpes simplex virus (HSV) encephalitis infections in animals. Iodination of 1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)cytosine X HCl (FAC X HCl) with Na 125I and NaI/HIO3 in aqueous acetic acid, and subsequent removal of residual iodine by CCl4 extraction and ion exchange chromatography, yielded [125I]FIAC in aqueous solution with a specific activity of 45.5 mCi/mmol in 44% radiochemical yield, and with a radiopurity of 96-97%. Methods for further purification are described.

摘要

已制备出1-(2-脱氧-2-氟-β-D-阿拉伯呋喃糖基)-5-碘胞嘧啶(FIAC)的125I标记类似物,用于研究动物单纯疱疹病毒(HSV)脑炎感染的成像。在乙酸水溶液中,用Na 125I和NaI/HIO3对1-(2-脱氧-2-氟-β-D-阿拉伯呋喃糖基)胞嘧啶盐酸盐(FAC·HCl)进行碘化,随后通过CCl4萃取和离子交换色谱法去除残留碘,得到[125I]FIAC水溶液,比活度为45.5 mCi/mmol,放射化学产率为44%,放射纯度为96 - 97%。文中描述了进一步纯化的方法。

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