Difluoro(methoxy)methyl Is a Neglected Group for Medicinal Chemistry─Revival via CF 2 OMe-Containing Amines

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.