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Updated: Jul 4, 2025

Protocol for the Synthesis of Ortho-trifluoromethoxylated Aniline Derivatives
Published on: January 19, 2016
Expanded Access to Fluoroformamidines via a Modular Synthetic Pathway
James A Vogel1, Kirya F Miller1, Eunjeong Shin1
1Department of Chemistry, Bryn Mawr College, Bryn Mawr, Pennsylvania 19010, United States.
Abstract:
Fluoroformamidines are an underutilized and understudied functional group despite combining two of the most highly prized elements in drug design: nitrogen and fluorine. We report a practical and modular synthesis of fluoroformamidines via the rearrangement of in situ-generated amidoximes. High yields in just 60 s at room temperature highlight the efficiency of this protocol. Furthermore, fluoroformamidines proved to be useful intermediates in the synthesis of diverse ureas and carbamimidates.
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