General Catalytic Methylation of Amines with Formic Acid under Mild Reaction Conditions

Abstract
A general catalytic protocol for the methylation of amines has been developed applying, for the first time, formic acid as the C1 building block and silanes as reducing agents. A broad range of aromatic and aliphatic, both primary and secondary, amines has been converted to the corresponding tertiary amines including [N13C]‐labelled drugs in good to excellent yields under mild conditions.