Electrochemical Synthesis of Phthalimidine‐d2 with Heavy Water as Deuterium Source

Advanced Synthesis and Catalysis(2023)

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摘要
Phthalimidine finds wide pharmaceutical applications and its deuterated derivative is supposed to exhibit enhanced stability towards metabolism. In this work, an electrochemically reductive deuteration strategy from phthalimide to phthalimidine-d(2) was achieved with D2O as a deuterium source at the reagent level in common solvents. This approach showed broad compatibility with a variety of functional groups. Mechanistic investigations assisted by electrochemical analysis revealed a 4-electron reduction pathway, and the coupled anodic oxygen evolution collectively maintains a neutral to mild basic conditions for the ongoing electrochemical reaction.
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关键词
deuterium source,synthesis
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