Metal-free intramolecular oxidative decarboxylative amination of primary α-amino acids with product selectivity

摘要

A novel metal-free intramolecular oxidative decarboxylative coupling of primary α-amino acids with 2-aminobenzoketones under mild and neutral conditions was developed. Different quinazolines can be selectively obtained by various oxidants. Transition metal-catalyzed decarboxylative couplings have emerged as important synthetic methods for C-C or C-N bond formation because of their high efficiency, selectivity and convenience.1 For instance, many chemists have developed transition metal-catalyzed intermolecular and intramolecular decarboxylative couplings, in which carboxylic acids or esters are directly employed as starting materials. A large number of coupling products - the intermediates for the synthesis of natural products - have been obtained. However, these decarboxylative couplings are restricted to the transition metal-assisted approach, requiring expensive transition metals, complex ligands and harsh reaction conditions.