中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
Divergent On-DNA Transformations from DNA-Linked Piperidones

文献类型:期刊论文

作者Ling, Xing1,4; Lu, Weiwei4; Miao, Lin2; Marcaurelle, Lisa A.3; Wang, Xuan4; Ding, Yun3; Lu, Xiaojie1,4
刊名JOURNAL OF ORGANIC CHEMISTRY
出版日期2022-02-18
卷号87期号:4页码:1971-1976
ISSN号0022-3263
DOI10.1021/acs.joc.1c00670
通讯作者Wang, Xuan(wangxuan2@simm.ac.cn) ; Ding, Yun(yun.x.ding@gsk.com) ; Lu, Xiaojie(xjlu@simm.ac.cn)
英文摘要A group of highly efficient and divergent transformations for constructing multiple DNA-linked chemotypes based on a piperidone core were successfully developed. We reported the first procedure for the synthesis of a DNA-conjugated piperidine intermediate under basic conditions. Subsequently, this substructure was subjected to additional reactions to generate several privileged scaffolds, including 4-aminopiperidine, fused [1,2,4]triazolo[1,5-a]pyrimidine, and a quinoline derivative. These transformations paved the way for constructing focused scaffold-based DNA-encoded libraries with druglike properties.
资助项目NSFC[21877117] ; NSFC[91953203] ; National Science & Technology Major Project Key New Drug Creation and Manufacturing Program, China[2018ZX09711002-005] ; Shanghai Commission of Science and Technology[18431907100] ; [NSFC-21907103]
WOS研究方向Chemistry
语种英语
出版者AMER CHEMICAL SOC
WOS记录号WOS:000762795100008
源URL[http://119.78.100.183/handle/2S10ELR8/300176]  
专题新药研究国家重点实验室
通讯作者Wang, Xuan; Ding, Yun; Lu, Xiaojie
作者单位1.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
2.Univ Nottingham Ningbo China, Ningbo 315100, Zhejiang, Peoples R China
3.GlaxoSmithKline, ELT NCE Mol Discovery, Med Sci & Technol, Cambridge, MA 02410 USA
4.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714
Ling, Xing,Lu, Weiwei,Miao, Lin,et al. Divergent On-DNA Transformations from DNA-Linked Piperidones[J]. JOURNAL OF ORGANIC CHEMISTRY,2022,87(4):1971-1976.
APA Ling, Xing.,Lu, Weiwei.,Miao, Lin.,Marcaurelle, Lisa A..,Wang, Xuan.,...&Lu, Xiaojie.(2022).Divergent On-DNA Transformations from DNA-Linked Piperidones.JOURNAL OF ORGANIC CHEMISTRY,87(4),1971-1976.
MLA Ling, Xing,et al."Divergent On-DNA Transformations from DNA-Linked Piperidones".JOURNAL OF ORGANIC CHEMISTRY 87.4(2022):1971-1976.

入库方式: OAI收割

来源:上海药物研究所

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