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Updated: Feb 20, 2026

Protocol for the Synthesis of Ortho-trifluoromethoxylated Aniline Derivatives
Published on: January 19, 2016
Recent advances in fluoride-free aryne generation from arene precursors
Fahima I M Idiris1, Christopher R Jones
1School of Biological and Chemical Sciences, Queen Mary University of London, Mile End Road, London, E1 4NS, UK. c.jones@qmul.ac.uk.
Abstract:
Aryne chemistry has experienced a remarkable renaissance in recent years, with a significant increase in the synthetic applications reported for these highly valuable reactive intermediates. This resurgence of interest is in part due to the introduction of ortho-silylaryl triflates as precursors which can be activated under mild conditions using fluoride. Alternative fluoride-free strategies have received interest in the last decade, with a number of precursors to arynes and their activators reported. These approaches offer alternative modes of reactivity which prove, in some cases, to be orthogonal to those of ortho-silylaryl triflates. This review highlights some of the more recent fluoride-free methodologies developed to access aryne intermediates that start from arene-based precursors.
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