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

来源：

ORGANIC LETTERS | 2024年 / 26卷 / 07期

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

页码：1353 / 1357

页数：5

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