A two-step, one-pot enzymatic synthesis of ampicillin from penicillin G potassium salt

作者：Du, Li-Li; Wu, Qi^*; Chen, Chun-Xiu; Liu, Bo-Kai; Lin, Xian-Fu

来源：Journal of Molecular Catalysis B: Enzymatic , 2009, 58(1-4): 208-211.

DOI：10.1016/j.molcatb.2008.12.020

• Penicillin acylase
• Ampicillin
• Enzymatic synthesis
• One-pot
• Penicillin G potassium

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 degrees 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 P-lactam antibiotics industry.

• 出版日期2009-6
• 单位浙江大学