N-methylation Reactions under Electrosynthesis Conditions

The methylation of nitrogenated molecules is of great relevance to access many organic molecules, including natural products and active pharmaceutical ingredients (APIs). Normally, N-methylation is performed using NaBH₄, H₂ and/or high-temperature conditions. Electrochemistry has recently introduced new synthetic methodologies, by replacing chemical reducing or oxidizing reagents with electrical energy.  We herein present a new approach to N-methylation via electrochemistry, for the development of a robust and efficient protocol for the synthesis of high-value APIs. Optimization studies based on the reaction between N-dibenzylamine and formaldehyde have successfully yielded the corresponding N-methylated molecule, in 51% yield so far. Further optimizations are under execution with positive perspectives of short-term improvements.