Zheng Shixin, Wang Dong, Huang Mindong, Yu Peng
College of Biotechnology, Tianjin University of Science and Technology, Tianjin, 300457, P. R. China.
State Key Laboratory of Chemistry and Utilization of Carbon Based Energy Resources, College of Chemistry, Xinjiang University, Urumqi, 830017, Xinjiang, P. R. China.
Chem Asian J. 2022 May 16;17(10):e202200077. doi: 10.1002/asia.202200077. Epub 2022 Apr 14.
A rapid, practical and scalable method for the reductant and tansition-metal-free synthesis of a variety of novel 2,4-disubstituted tetrahydropyridines and tetrahydroquinolines is disclosed. The method is based upon dearomative functionalization of pyridines or quinolines to generate amino nitrile intermediates as masked iminium ions, which then react rapidly with various Grignard reagents in complete stereocontrol.
公开了一种用于多种新型2,4-二取代四氢吡啶和四氢喹啉的无还原剂和过渡金属合成的快速、实用且可扩展的方法。该方法基于吡啶或喹啉的去芳构化官能化以生成作为掩蔽亚胺离子的氨基腈中间体，然后这些中间体在完全立体控制下与各种格氏试剂快速反应。
