Synthesis of deuterium-labeled 1-(4-methoxybenzyl)-3-(5-nitrothiazol-2-yl)urea (AR-A014418) as an internal standard for LC-MS analysis

被引：2
|
作者：
Liang, Dawei [1 ]
Wang, Yueqiu [1 ]
Yan, Tingchang [2 ]
Wang, Zhaoyang [2 ]
机构：
[1] Yaan Polytech Coll, Sch Pharm & Med Lab Sci, Yaan 625000, Sichuan, Peoples R China
[2] Shandong Huijing Biopharmaceut Technol Co Ltd, 1 Lutai Rd, Zibo 255000, Shandong, Peoples R China
来源：
JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY | 2020年 / 325卷 / 01期
关键词：
Deuterium labeling; AR-A014418; Internal standard; Synthesis; SYNTHASE; INHIBITION; SUPPRESSES;
D O I：
10.1007/s10967-020-07227-0
中图分类号：
O65 [分析化学];
学科分类号：
070302 ; 081704 ;
摘要：
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 [H-2(3)]AR-A014418 was synthesized in seven steps with 21% overall yield starting from the commercially available [H-2(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 [H-2(3)]AR-A014418 can be used as an internal standard for LC-MS analysis in drug absorption, distribution and other pharmacokinetics studies. [GRAPHICS] .
引用
收藏
页码：217 / 222
页数：6
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