School of Chemistry, Chemical Engineering and Life Sciences, Wuhan University of Technology, Wuhan 430070, China.
Shenzhen Research Institute, Wuhan University of Technology, Shenzhen, Guangdong 518057, China.
Org Lett. 2021 May 21;23(10):3923-3927. doi: 10.1021/acs.orglett.1c01083. Epub 2021 May 3.
2-Fluoro-5-(trifluoromethyl)aniline was found to be a suitable monodentate transient directing group (MonoTDG) to enable Ru(II)-catalyzed intermolecular direct -C(sp)-H imidation of benzaldehydes. -Tosyloxyphthalimide was used as an alternative azide-free amidation reagent to achieve high efficiency and good functional group tolerance. Moreover, the reaction could be enlarged to gram scale, and the amidated product could be readily converted into useful quinazoline and fused isoindolinone scaffolds by one-step derivatization.
2-氟-5-(三氟甲基)苯胺被发现是一种合适的单齿瞬态导向基团（MonoTDG），可使 Ru(II)催化的苯甲醛间直接 -C(sp)-H 亚胺化反应得以进行。-对甲苯磺酰氧基邻苯二甲酰亚胺被用作替代无叠氮酰胺化试剂，以实现高效率和好的官能团耐受性。此外，该反应可以放大到克级规模，并且酰胺化产物可以通过一步衍生化很容易转化为有用的喹唑啉和稠合异吲哚啉酮骨架。
