Efficient and Practical Synthesis of 3 ',4 ',5 '-Trifluoro-[1,1 '-biphenyl]-2-amine: A Key Intermediate of Fluxapyroxad

摘要

An improved and practical method is reported here for accessing 3',4',5'-trifluoro-[1,1'-biphenyl]-2-amine (1), a key intermediate for Fluxapyroxad. The overall yield for the preparation of 1 was 73%, with a purity of 99.88%, after a three-step process. More importantly, this process was an improvement in the manufacture of biphenyl compounds by Suzuki-Miyaura coupling, which enabled catalyst loading as low as 0.04 mol %. This method could provide an economic and environment friendly process leading to extensive prospects in industrial applications.