Synthesis of Polysubstituted Trifluoromethyl Pyridines from Trifluoromethyl-α,β-ynones.

Research paper by Tianyu T Yang, Zhoubin Z Deng, Ke-Hu KH Wang, Pengfei P Li, Danfeng D Huang, Yingpeng Y Su, Yulai Y Hu

Indexed on: 15 Dec '19Published on: 14 Dec '19Published in: Journal of Organic Chemistry


A novel and efficient method for synthesis of polysubstituted trifluoromethylpyridine derivatives by Bohlmann-Rahtz heteroannulation reaction is described, which use trifluoromethyl-α,β-ynones as trifluoromethyl building block to react with β-enamino esters or β-enamino ketones in the presence of ZnBr2 to form the trifluoromethylpyridine derivatives in good yields. The protocol has the advantages of readily available starting materials, mild reaction conditions and high atom economy.