Dithiol Aryl Arsenic Compounds as Potential Diagnostic and Therapeutic Radiopharmaceuticals

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• 作者：Anthony J. DeGraffenreid ; Yutian Feng ; Donald E. Wycoff ; Ryan Morrow ; Michael D. Phipps ; Cathy S. Cutler ; Alan R. Ketring ; Charles L. Barnes ; Silvia S. Jurisson
• 刊名：Inorganic Chemistry
• 出版年：2016
• 出版时间：August 15, 2016
• 年：2016
• 卷：55
• 期：16
• 页码：8091-8098
• 全文大小：394K
• 年卷期：0
• ISSN：1520-510X

文摘

Arsenic-72 (⁷²As) and ⁷⁷As have nuclear properties useful for positron emission tomography (PET) and radiotherapy, respectively. The thiophilic nature of arsenic led to the evaluation of dithioarylarsines for potential use in radiopharmaceuticals. Several dithioarylarsines were synthesized from their arylarsonic acids and dithiols and were fully characterized by NMR, ESI-MS, and X-ray crystallography. This chemistry was translated to the no-carrier-added (nca) ⁷⁷As level. Because arsenic was available at the nca nanomolar level only as [⁷⁷As]arsenate, this required addition of an aryl group directly to the As to form the [⁷⁷As]arylarsonic acid. The [⁷⁷As]arsenate was reduced from ⁷⁷As (V) to ⁷⁷As (III), and a modified Bart reaction was used to incorporate the aryl ring onto the ⁷⁷As, which was followed by dithiol addition. Various modifications and optimizations resulted in 95% radiochemical yield of nca [⁷⁷As]p-ethoxyphenyl-1,2-ethanedithiolatoarsine.