A two-step, one-pot enzymatic synthesis of ampicillin from penicillin G potassium salt |
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Authors: | Li-Li Du Qi Wu Chun-Xiu Chen Bo-Kai Liu Xian-Fu Lin |
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Institution: | aDepartment of Chemistry, Zhejiang University, Hangzhou 310027, People's Republic of China |
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Abstract: | A two-step, one-pot synthesis of ampicillin from penicillin G potassium salt (PGK) in aqueous buffer/organic co-solvent has been achieved. Ethylene glycol (EG) was chosen as the organic co-solvent. Factors including co-solvent content, enzyme loading, reaction temperature and substrate concentration were investigated. The optimum conditions were as follow: pH 8.0 phosphate buffer solution, 50% EG (v/v), 25 °C, 100 mM PGK and 300 mM d-phenylglycine methyl ester (D-PGM), 43.2 IU/ml IPA-750. The maximum yield was 57.3% after a reaction time of 17 h. It is the first report about the synthesis of ampicillin from penicillin G potassium salt in one-pot combining the enzymatic hydrolysis and the subsequent enzymatic condensation, and the novel methodology will have important application in the β-lactam antibiotics industry. |
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Keywords: | Penicillin acylase Ampicillin Enzymatic synthesis One-pot Penicillin G potassium |
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