末端炔烃的DNA兼容氧化与酰胺化反应
DNA Compatible Oxidization and Amidation of Terminal Alkynes.
作者信息
Sun Zhaomei, Zhang Jie, Zhang Huanqing, Cao Hongli, Xiao Lingqian, Yang Kexin, Hu Yun Jin
机构信息
Pharmaron (Ningbo) Technology Development Co., Ltd., No. 800 Bin-Hai 4th Road, Hangzhou Bay New Zone, Ningbo, 315336, China.
Pharmaron Beijing Co., Ltd., 6 Taihe Road, BDA, Beijing, 100176, China.
出版信息
Bioconjug Chem. 2022 Sep 21;33(9):1585-1594. doi: 10.1021/acs.bioconjchem.2c00340. Epub 2022 Aug 24.
Through a modified Kinugasa reaction, a novel method of amidation on terminal oligo alkyne conjugates by copper-promoted oxidation with nitrones has been developed. Unprotected bifunctional carboxylic acid-amine reagents can be transformed directly to the respective amide products under these edited Kinugasa reaction conditions. 3-Cycle DNA-encoded libraries (DELs) can be built in three steps of chemical conversion.
通过改良的衣笠反应，开发了一种通过铜促进的硝酮氧化对末端寡炔共轭物进行酰胺化的新方法。在这些经过编辑的衣笠反应条件下，未受保护的双功能羧酸 - 胺试剂可直接转化为相应的酰胺产物。3 - 环DNA编码文库（DELs）可以通过三步化学转化构建。
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