Abstract AR-A014418, 1-(4-methoxybenzyl)-3-(5-nitrothiazol-2-yl)urea is a potential drug with potent activities against cancer cell, nociceptive pain and neurodegenerative disorders. In this paper, the stable deuterium-labeled [ 2 H 3 ]AR-A014418 was synthesized in seven steps with 21% overall yield starting from the commercially available [ 2 H 4 ]methanol, p -hydroxybenzaldehyde and 2-amino-5-nitrothiazole. The chemical and isotope purity of the title compound were over 99% and 98%, respectively. This labeled [ 2 H 3 ]AR-A014418 can be used as an internal standard for LC–MS analysis in drug absorption, distribution and other pharmacokinetics studies. Graphic abstract

中文翻译：

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合成氘标记的 1-(4-甲氧基苄基)-3-(5-硝基噻唑-2-基)脲 (AR-A014418) 作为 LC-MS 分析的内标

摘要 AR-A014418，1-(4-甲氧基苄基)-3-(5-硝基噻唑-2-基)脲是一种潜在的药物，对癌细胞、伤害性疼痛和神经退行性疾病具有有效的活性。在本文中，以市售的[ 2 H 4 ]甲醇、对羟基苯甲醛和2-氨基-5-硝基噻唑为原料，分七步合成了稳定的氘标记的[ 2 H 3 ]AR-A014418，总产率为21%。 . 标题化合物的化学和同位素纯度分别超过 99% 和 98%。这种标记的 [ 2 H 3 ]AR-A014418 可用作药物吸收、分布和其他药代动力学研究中 LC-MS 分析的内标。图形摘要