The paper presents an analytical review of the literature on enzymatic synthesis of semisynthetic beta-lactam antibiotics. The results of the studies on the thermodynamics and kinetics of beta-lactams synthesis are generalized and the approaches to increasing the efficiency of the biocatalytic processes based on both thermodynamically controlled synthesis (direct) and kinetically controlled synthesis (acyl transfer) are systematized. Characteristic features of the processes for separation of the reaction mass components and recovery of the final products of the biocatalytic synthesis of beta-lactam antibiotics are considered and the pathways to increasing the economic efficiency of biocatalytic processes used in design of the technologies and their introduction to manufacture are discussed.

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