Abstract
AbstractFluorinated 1‐benzoyl‐3,4‐dihydroisoquinolines can easily be synthesized by a new one‐pot procedure from corresponding fluorinated [2‐(o‐alkynylphenyl)ethyl]amines in high yields. The one‐pot process consists of an initial [Ind2TiMe2]‐catalyzed intramolecular alkyne hydroamination and a subsequent Pd‐catalyzed oxidation of the benzyl side chain of the resulting hydroamination product. The process tolerates electron‐donating and ‐withdrawing substituents on the benzene ring that is converted into the benzoyl side chain of the products as well as ortho‐substitution.
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