作者:Mizuno, Shota、Yotsume, Futa、Kasahara, Runa、Inoue, Munenori、Ichikawa, Junji、Fujita, Takeshi
DOI:10.1002/adsc.202400508
日期:——
The synthesis of indoles with a trifluoromethyl group has attracted a lot of attention because they are promising structural subunits for pharmaceuticals and agrochemicals. As part of our project aimed toward the upcycling of hydrofluoroolefins (HFOs), we developed a method to construct a CF3‐bearing indole ring system through the Suzuki–Miyaura cross‐coupling of a brominated HFO‐1234ze(E) (CF3CH=CHF)
具有三氟甲基的吲哚的合成引起了广泛的关注,因为它们是有前途的药物和农用化学品的结构亚基。作为我们旨在氢氟烯烃 (HFO) 升级循环的项目的一部分,我们开发了一种通过溴化 HFO 的 Suzuki-Miyaura 交叉偶联构建 CF3 轴承吲哚环系统的方法‐1234ze(E) (CF3CH=CHF) 与 N-甲苯磺酰化 o-硼基苯胺,然后在生成的氟苯乙烯的乙烯基位置上进行亲核 5-endo-trig 环化。我们发现Pd2(dba)3/SPhos催化剂体系在K2CO 和水的甲苯溶液在一锅操作中以高产率提供了相应的 3-CF3-吲哚。