Li Xuming, Ye Xiaohan, Wei Chiyu, Shan Chuan, Wojtas Lukasz, Wang Qilin, Shi Xiaodong
The Department of Chemistry, University of South Florida, 4202 East Fowler Avenue, Tampa, Florida 33620, United States.
Institute of Functional Organic Molecular Engineering, College of Chemistry and Chemical Engineering, Henan University, Kaifeng 475004, China.
Org Lett. 2020 Jun 5;22(11):4151-4155. doi: 10.1021/acs.orglett.0c01232. Epub 2020 May 28.
A donor/acceptor diazo activation strategy, processing via condensation using diazonium salts without the addition of any other catalysts or reagents, is reported. The diazenium intermediate was found to undergo cyclization to give indazoles in excellent yields. Alternatively, in the presence of nitriles, substituted 1,2,4-triazoles were obtained in good to excellent yields. This interesting diazenium route provides a new approach to achieve complex heterocycle synthesis under mild conditions.
报道了一种供体/受体重氮活化策略，该策略通过使用重氮盐进行缩合反应来进行，无需添加任何其他催化剂或试剂。发现重氮鎓中间体可进行环化反应，以优异的产率得到吲唑。另外，在腈存在的情况下，可获得产率良好至优异的取代1,2,4-三唑。这种有趣的重氮鎓路线为在温和条件下实现复杂杂环合成提供了一种新方法。
