DOI: 10.1002/slct.74636 ISSN: 2365-6549
Efficient Three‐Component Cyanation Synthesis of Quinoline Under Solvent‐Free and Additive‐Free Conditions
Xujin Zhang, Lihua Huang, Jiankun Chen, Wenxin Zhang, Yongbiao Guo, Xiandong Dai, Zirui Lv, Chunru Cheng, Fanhua Meng, Zhenhua GaoABSTRACT
An efficient dearomative cyanidation of quinoline is described, which enables the synthesis of a series of α‐cyanoquinolines under solvent‐free and additive‐free conditions (29 examples, yield up to 99%). By using low‐toxicity and commercially available starting materials, this method allows for direct α‐position cyanation, exhibiting broad functional group compatibility and excellent scalability for gram‐scale (10 mmol, 97% yield) synthesis with consistently high yields. Furthermore, the different reaction pathways that lead to the experimentally observed products were investigated through DFT calculations and NMR studies.