The coupling in aqueous systems between N-carboxyanhydrides of amino acids (NCA's) and amino acids such as 6-arninopenicillanic acid (6-APA) can be controlled to give high yields of dipeptide. Minimization of rearrangement, polymerization, and hydrolysis reactions depends upon selection of a pH level and ratio of reactant concentrations capable of maintaining the total base strength of attacking 6-APA, established by both the pK2 and ...