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DOI | 10.1126/science.aap9674 |
Photoredox-catalyzed deuteration and tritiation of pharmaceutical compounds | |
Loh, Yong Yao1; Nagao, Kazunori1; Hoover, Andrew J.2; Hesk, David2; Rivera, Nelo R.2; Colletti, Steven L.3; Davies, Ian W.1,2; MacMillan, David W. C.1 | |
2017-12-01 | |
发表期刊 | SCIENCE
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ISSN | 0036-8075 |
EISSN | 1095-9203 |
出版年 | 2017 |
卷号 | 358期号:6367页码:1182-+ |
文章类型 | Article |
语种 | 英语 |
国家 | USA |
英文摘要 | Deuterium- and tritium-labeled pharmaceutical compounds are pivotal diagnostic tools in drug discovery research, providing vital information about the biological fate of drugs and drug metabolites. Herein we demonstrate that a photoredox-mediated hydrogen atom transfer protocol can efficiently and selectively install deuterium (D) and tritium (T) at a-amino sp(3) carbon-hydrogen bonds in a single step, using isotopically labeled water (D2O or T2O) as the source of hydrogen isotope. In this context, we also report a convenient synthesis of T2O from T-2, providing access to high-specific-activity T2O. This protocol has been successfully applied to the high incorporation of deuterium and tritium in 18 drug molecules, which meet the requirements for use in ligand-binding assays and absorption, distribution, metabolism, and excretion studies. |
领域 | 地球科学 ; 气候变化 ; 资源环境 |
收录类别 | SCI-E |
WOS记录号 | WOS:000416584000041 |
WOS关键词 | BOND-DISSOCIATION ENERGIES ; HYDROGEN ISOTOPE-EXCHANGE ; DRUG DISCOVERY ; AMINES ; DESIGN ; STABILIZATION ; ACTIVATION ; COMPLEXES ; CHEMISTRY ; RHODIUM |
WOS类目 | Multidisciplinary Sciences |
WOS研究方向 | Science & Technology - Other Topics |
URL | 查看原文 |
引用统计 | |
文献类型 | 期刊论文 |
条目标识符 | http://119.78.100.173/C666/handle/2XK7JSWQ/197433 |
专题 | 地球科学 资源环境科学 气候变化 |
作者单位 | 1.Princeton Univ, Merck Ctr Catalysis, Princeton, NJ 08544 USA; 2.Merck & Co Inc, Merck Res Labs, Dept Proc R&D, Labeled Compound Synth Grp, Rahway, NJ 07065 USA; 3.Merck & Co Inc, MRL, Dept Discovery Chem, Kenilworth, NJ 07033 USA |
推荐引用方式 GB/T 7714 | Loh, Yong Yao,Nagao, Kazunori,Hoover, Andrew J.,et al. Photoredox-catalyzed deuteration and tritiation of pharmaceutical compounds[J]. SCIENCE,2017,358(6367):1182-+. |
APA | Loh, Yong Yao.,Nagao, Kazunori.,Hoover, Andrew J..,Hesk, David.,Rivera, Nelo R..,...&MacMillan, David W. C..(2017).Photoredox-catalyzed deuteration and tritiation of pharmaceutical compounds.SCIENCE,358(6367),1182-+. |
MLA | Loh, Yong Yao,et al."Photoredox-catalyzed deuteration and tritiation of pharmaceutical compounds".SCIENCE 358.6367(2017):1182-+. |
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