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 [N-(13)C]-labelled drugs in good to excellent yields under mild conditions.