Hickey Michael J, Allen Paul H, Caffrey Moya, Hansen Peter, Kingston Lee P, Wilkinson David J
Drug Safety and Metabolism, Innovative Medicines and Early Development Biotech Unit, AstraZeneca, Cambridge, UK.
Respiratory, Inflammation and Autoimmunity, Innovative Medicines and Early Development Biotech Unit, AstraZeneca, Gothenburg, Sweden.
J Labelled Comp Radiopharm. 2016 Sep;59(11):432-8. doi: 10.1002/jlcr.3429. Epub 2016 Jul 27.
The CXCR2 antagonist AZD5069 has been synthesized in tritium and carbon-14-labelled forms. [(3) H]AZD5069 was prepared via reductive dehalogenation of an iodinated precursor with tritium gas to provide material with a specific activity of 25.1 Ci/mmol. [(14) C]AZD5069 was labelled in the pyrimidine ring from [(14) C]thiourea in an overall radiochemical yield of 18%. In addition, a synthetic route to the major metabolite of AZD5069 was developed. The synthesis of this metabolite was achieved from AZD5069 using a chemoselective Lindgren-Pinnick reaction in order to minimize oxidation of the sulphide group.
CXCR2拮抗剂AZD5069已被合成出氚标记和碳-14标记的形式。[³H]AZD5069是通过用氚气对碘化前体进行还原脱卤制备的，得到的材料比活度为25.1居里/毫摩尔。[¹⁴C]AZD5069是由[¹⁴C]硫脲在嘧啶环上标记的，总放射化学产率为18%。此外，还开发了一条合成AZD5069主要代谢物的路线。该代谢物的合成是从AZD5069出发，使用化学选择性的林德格伦-平尼克反应，以尽量减少硫醚基团的氧化。
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