State Key Laboratory of Materials-Oriented Chemical Engineering, College of Chemical Engineering , Nanjing Tech University , Nanjing 211800 , China.
Org Lett. 2019 Jun 7;21(11):4148-4152. doi: 10.1021/acs.orglett.9b01334. Epub 2019 May 15.
Pyridotriazoles are utilized as robust building blocks to access α-secondary and α-tertiary pyridines via the development of a simple yet practically useful metal-free denitrogenative C-C cross-coupling with boronic acids. The reaction shows a high level of functional tolerance, broad substrate scope, and facile scalability. The synthetic potential of the method is demonstrated by the strurctural modification of a bioactive molecule and concise synthesis of pheniramine analogs.
哒嗪三唑被用作构建模块，通过开发一种简单而实用的无金属脱氮 C-C 交叉偶联与硼酸反应，来获得α-仲位和α-叔位吡啶。该反应具有高水平的官能团容忍度、广泛的底物范围和易于扩大规模的特点。该方法的合成潜力通过对生物活性分子的结构修饰和苯海拉明类似物的简洁合成得到了证明。
