Efficient synthesis of cefadroxil in [Bmim][NTf2]‐phosphate cosolvent by magnetic immobilized penicillin G acylase,Journal of the Chinese Chemical Society

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Efficient synthesis of cefadroxil in [Bmim][NTf2]‐phosphate cosolvent by magnetic immobilized penicillin G acylase
Journal of the Chinese Chemical Society ( IF 1.6 ) Pub Date : 2019-10-17 , DOI: 10.1002/jccs.201900272
Zheng Zhaoyu ₁ , Hu Chunmiao ₁ , Du Chuanhu ₁ , Xue Ping ₁ , Zhang Weiwei ₁

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For the first time, cefadroxil was synthesized from 7‐Amino‐3‐desacetoxycephalosporanic acid and d‐hydroxyphenylglycine methyl ester in [Bmim][NTf₂]‐phosphate cosolvent capable of dissolving the substrates using the penicillin G acylase (PGA) immobilized on the micrometer‐size magnetic polymer microspheres having high activity of 2,083 U/g. The high synthesis/hydrolysis (S/H) ratio of 1.12 was achieved with 79.0% yield, where only the S/H ratio of 0.19 and yield of 20.0% was obtained using free PGA under the identical optimum reaction conditions. Cefadroxil had been synthesized efficiently in [Bmim][NTf₂]‐phosphate cosolvent by the magnetic immobilized PGA, which illuminated that there are two very critical and essential designs, that is, effective support and suitable solvent system by PGA, in enzymatic synthesis of cefadroxil. Obviously, there is great potential for the magnetic immobilized PGA and ionic liquid solvent in application to biocatalysis.

中文翻译：

磁性固定化青霉素G酰基转移酶在[Bmim] [NTf2]-磷酸酯助溶剂中高效合成头孢氨苄

头孢氨苄首次由7-氨基-3-去乙酰氧基头孢菌酸和d-羟苯基甘氨酸甲酯在[Bmim] [NTf ₂ ]-磷酸酯助溶剂中合成，能够使用固定在其上的青霉素G酰基转移酶（PGA）溶解底物。微米级磁性聚合物微球，具有2,083 U / g的高活性。在相同的最佳反应条件下，使用游离PGA仅获得了1.12的高合成/水解（S / H）比和79.0％的收率，其中只有0.19的S / H比和20.0％的收率得到了。在[Bmim] [NTf ₂磁性固定的PGA产生的]-磷酸酯助溶剂，表明头孢氨苄的酶法合成中有两个非常关键且必不可少的设计，即有效的支持和PGA合适的溶剂体系。显然，磁性固定的PGA和离子液体溶剂在生物催化中具有很大的潜力。

更新日期：2019-12-11

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