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DOI | 10.1126/science.aam7936 |
A multifunctional catalyst that stereoselectively assembles prodrugs | |
DiRocco, Daniel A.; Ji, Yining; Sherer, Edward C.; Klapars, Artis; Reibarkh, Mikhail; Dropinski, James; Mathew, Rose; Maligres, Peter; Hyde, Alan M.; Limanto, John; Brunskill, Andrew; Ruck, Rebecca T.; Campeau, Louis-Charles; Davies, Ian W. | |
2017-04-28 | |
发表期刊 | SCIENCE |
ISSN | 0036-8075 |
EISSN | 1095-9203 |
出版年 | 2017 |
卷号 | 356期号:6336页码:426-429 |
文章类型 | Article |
语种 | 英语 |
国家 | USA |
英文摘要 | The catalytic stereoselective synthesis of compounds with chiral phosphorus centers remains an unsolved problem. State-of-the-art methods rely on resolution or stoichiometric chiral auxiliaries. Phosphoramidate prodrugs are a critical component of pronucleotide (ProTide) therapies used in the treatment of viral disease and cancer. Here we describe the development of a catalytic stereoselective method for the installation of phosphorus-stereogenic phosphoramidates to nucleosides through a dynamic stereoselective process. Detailed mechanistic studies and computational modeling led to the rational design of a multifunctional catalyst that enables stereoselectivity as high as 99:1. |
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:000400143000051 |
WOS关键词 | KINETIC RESOLUTION ; ENANTIOSELECTIVE SYNTHESIS ; FACILE SYNTHESIS ; ENZYME-ACTIVITY ; NUCLEOSIDE ; PHOSPHORYLATION ; PHOSPHATE ; DISCOVERY ; ANALOGS |
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/195925 |
专题 | 地球科学 资源环境科学 气候变化 |
作者单位 | Merck & Co Inc, Proc Res & Dev, Rahway, NJ 07065 USA |
推荐引用方式 GB/T 7714 | DiRocco, Daniel A.,Ji, Yining,Sherer, Edward C.,et al. A multifunctional catalyst that stereoselectively assembles prodrugs[J]. SCIENCE,2017,356(6336):426-429. |
APA | DiRocco, Daniel A..,Ji, Yining.,Sherer, Edward C..,Klapars, Artis.,Reibarkh, Mikhail.,...&Davies, Ian W..(2017).A multifunctional catalyst that stereoselectively assembles prodrugs.SCIENCE,356(6336),426-429. |
MLA | DiRocco, Daniel A.,et al."A multifunctional catalyst that stereoselectively assembles prodrugs".SCIENCE 356.6336(2017):426-429. |
条目包含的文件 | 条目无相关文件。 |
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