Synthesis of Thiohydantoin Scaffolds on DNA for Focused DNA-Encoded Library Construction

被引:1
|
作者
Fang, Xianfu [1 ,2 ]
Ju, Yunzhu [1 ]
Wang, Jiayou [1 ]
Zhang, Gong [1 ]
Li, Yangfeng [1 ]
Li, Yizhou [1 ]
机构
[1] Chongqing Univ, Innovat Drug Res Ctr, Sch Pharmaceut Sci, Chongqing Key Lab Nat Prod Synth & Drug Res, Chongqing 401331, Peoples R China
[2] Chongqing Univ, Pharmaceut Dept, Gorges Hosp 3, Chongqing 404100, Peoples R China
基金
中国国家自然科学基金;
关键词
DISCOVERY; DRUGS;
D O I
10.1021/acs.orglett.4c03369
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Thiohydantoin represents a significant class of biologically active privileged heterocyclic scaffolds. Herein, we present a convenient and robust DNA-compatible method for constructing a thiohydantoin-focused DNA-encoded library. This reaction can be applied to a wide variety of isothiocyanate partners, arylamine feedstocks, and diverse alpha-amine acid derivatives, exhibiting excellent conversions, high functional group tolerance, and preservation of DNA tag integrity. Our method allows for easy access to a valuable three-cycle thiohydantoin-focused DNA-encoded library.
引用
收藏
页码:8916 / 8921
页数:6
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