A mild and efficient method for the monocarboxymethylation of primary amines that takes place under aq. conditions at room temp. is described. Treatment of an aq. soln. of a variety of primary amines with two equiv. of glyoxylic acid leads to the N-formyl glycine derivs. Direct hydrolysis of the crude reaction soln. leads to the products of amine monocarboxymethylation in good to excellent yield.
- one-pot monocarboxymethylation
- primary amines