Efficient and Practical Synthesis of 3′,4′,5′-Trifluoro-[1,1′-biphenyl]-2-amine: A Key Intermediate of Fluxapyroxad,Organic Process Research & Development

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Efficient and Practical Synthesis of 3′,4′,5′-Trifluoro-[1,1′-biphenyl]-2-amine: A Key Intermediate of Fluxapyroxad
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2019-08-14 00:00:00 , DOI: 10.1021/acs.oprd.9b00208
Zhenhua Li _{1,

2} , Xuchao Zhang ₁ , Jinjing Qin ₁ , Zhiyong Tan ₁ , Meizhen Han ₂ , Guoqiang Jin ₁

Affiliation

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.

中文翻译：

高效实用合成3'，4'，5'-三氟-[1,1'-联苯] -2-胺：氟哌啶的关键中间体

在此报道了一种改进的实用方法，用于获得3'，4'，5'-三氟-[1,1'-联苯] -2-胺（1），这是氟虫嘧啶的关键中间体。经三步法处理后，制备1的总产率为73％，纯度为99.88％。更重要的是，该工艺是通过Suzuki-Miyaura偶联生产联苯化合物的一项改进，使催化剂的负载量低至0.04 mol％。该方法可以提供经济和环境友好的方法，从而在工业应用中具有广阔的前景。

更新日期：2019-08-14

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