One-step method for synthesizing amoxicillin from penicillin or salt thereof through enzyme catalysis

Abstract

A one-step method for synthesizing amoxicillin from penicillin or a salt thereof through an enzyme catalysis is provided. Conventional amoxicillin production requires sequential use of distinct penicillin acylases for hydrolysis and synthesis steps, necessitating isolation of the intermediate 6-aminopenicillanic acid (6-APA) and resulting in elevated manufacturing costs and suboptimal process efficiency. To address these limitations, the inventive method utilizes a mutant of penicillin acylase derived from Kluyvera citrophila as the exclusive biocatalyst in an aqueous reaction system. By reacting penicillin G potassium salt with D-p-hydroxyphenylglycine methyl ester, the process achieves direct amoxicillin synthesis in a single enzymatic step, attaining a product yield of 99%. This method exhibits advantages including fast catalytic rate, high product yield, environmentally friendly pure aqueous reaction system, low cost, and excellent economic benefits.

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