DNA-Compatible Cyclization Reaction to Access 1,3,4-Oxadiazoles and 1,2,4-Triazoles

被引:1
|
作者
Wang, Gaonan [1 ]
Tan, Yu [1 ]
Zou, Hanzhi [1 ]
Sui, Xihang [1 ]
Wang, Zhanlong [1 ]
Satz, Alexander L. [2 ]
Kuai, Letian [3 ]
Su, Wenji [1 ]
Zhang, Qi [1 ]
机构
[1] WuXi AppTec, Shanghai 200131, Peoples R China
[2] WuXi AppTec, D-82152 Martinsried, Germany
[3] WuXi AppTec, Cambridge, MA 02142 USA
关键词
D O I
10.1021/acs.orglett.3c04240
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
DNA-encoded chemical library (DECL) technology is a commonly employed screening platform in both the pharmaceutical industry and academia. To expand the chemical space of DECLs, new and robust DNA-compatible reactions are sought after. In particular, DNA-compatible cyclization reactions are highly valued, as these reactions tend to be atom economical and thus may provide lead- and drug-like molecules. Herein, we report two new methodologies employing DNA-conjugated thiosemicarbazides as a common precursor, yielding highly substituted 1,3,4-oxadiazoles and 1,2,4-triazoles. These two novel DNA-compatible reactions feature a high conversion efficiency and broad substrate scope under mild conditions that do not observably degrade DNA.
引用
收藏
页码:1353 / 1357
页数:5
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