A Mild and Efficient Method for the One-Pot Monocarboxymethylation of Primary Amines

Abstract

A mild and efficient method for the monocarboxymethylation of primary amines that takes place under aqueous conditions at room temperature is described. Treatment of an aqueous solution of a variety of primary amines with two equivalents of glyoxylic acid leads to the N-formyl glycine derivatives. Direct hydrolysis of the crude reaction solution leads to the products of amine mono­carboxymethylation in good to excellent yield.

metal-free synthesis - amino acids - glycine derivatives

References and Notes

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