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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