Organic Letters p. 3923 - 3927 (2021)
Update date:2022-08-04
Topics:
Wu, Yongdi
Liu, Na
Qi, Meifang
Qiao, Huihao
Lu, Xuelian
Ma, Li
Zhou, Yirong
Zhang, Fang-Lin
2-Fluoro-5-(trifluoromethyl)aniline was found to be a suitable monodentate transient directing group (MonoTDG) to enable Ru(II)-catalyzed intermolecular direct ortho-C(sp2)-H imidation of benzaldehydes. N-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.
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