Ding Dong, Liu Gang, Xu Guangyang, Li Jian, Wang Guoping, Sun Jiangtao
School of Pharmaceutical Engineering & Life Science, Changzhou University, Changzhou 213164, P. R. China.
Org Biomol Chem. 2014 Apr 28;12(16):2533-7. doi: 10.1039/c4ob00001c.
The palladium catalyzed carbenoid based N-H insertion and electronic effect controlled 5-exo-trig or 6-endo-trig mode Heck cyclization in one-pot has been realized for ortho-iodoanilines, in which PdCl2 was used as the single palladium resource. The corresponding indoles and quinolines were obtained respectively. However, for ortho-triflateanilines, base promoted cyclization is preferred and the lactones were obtained.
以邻碘苯胺为原料，实现了一锅法中钯催化的基于类卡宾的N-H插入反应以及电子效应控制的5-外式-三取代或6-内式-三取代模式的Heck环化反应，其中PdCl₂用作单一钯源。分别得到了相应的吲哚和喹啉。然而，对于邻三氟甲磺酸苯胺，碱促进的环化反应更有利，得到的是内酯。
