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Updated: May 24, 2026

Protocol for the Synthesis of Ortho-trifluoromethoxylated Aniline Derivatives
Published on: January 19, 2016
Scope of direct arylation of fluorinated aromatics with aryl sulfonates
Joyce Wei Wei Chang1, Eugene Yurong Chia, Christina Li Lin Chai
1Institute of Chemical and Engineering Sciences, 8 Biomedical Grove, Neuros, #07-01, Singapore 138665, Singapore.
Abstract:
The scope and limitations of direct arylation of fluorinated aromatics with aryl sulfonates was examined. Pd(OAc)(2), in the presence of MePhos and KOAc in THF, efficiently catalyzed the direct arylation of fluoro aromatics with aryl triflates under ambient conditions. Sterically hindered triflates and heteroaryl triflates gave good to excellent yields of the cross coupled products using a modified catalyst system which involves Pd(OAc)(2)-RuPhos at 100 °C. The direct arylation of electron deficient arenes with aryl mesylates is also established using Pd(OAc)(2)-SPhos as the catalyst in toluene-(t)BuOH at 120 °C.
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