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Updated: Mar 20, 2026

Protocol for the Synthesis of Ortho-trifluoromethoxylated Aniline Derivatives
Published on: January 19, 2016
Difluoro(methoxy)methyl Is a Neglected Group for Medicinal Chemistry─Revival via CF2OMe-Containing Amines
Mykhailo O Pashko1,2, Dmitry S Granat1,3, Oleksii O Klymenko-Ulianov3,4
1Enamine Ltd., 78 Winston Churchill str., 02094 Kyiv, Ukraine.
Abstract:
An efficient, scalable approach to CF2OMe-containing amines is reported. The scope and limitations of the reaction are delineated, including the influence of structural features and the nature of the protection group. The resulting CF2OMe amines are compatible with common synthetic transformations and exhibit favorable stability in plastic containers. These findings, along with measured physicochemical parameters, demonstrate the prospects of the CF2OMe group as an interesting motif for medicinal chemistry and agrochemical research.
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