酶法合成头孢羟氨苄工艺研究
发布时间：2019-06-09 17:47
【摘要】：对酶法合成头孢羟氨苄的工艺条件进行优化,以7-氨基-3-脱乙酰氧基头孢烷酸(7-amino-3-desacetoxy cephalosporanic acid,7-ADCA)为母核,对羟基苯甘氨酸甲酯(D-hydroxy phenylglycine methyl ester,D-HPGM)为酰基供体,利用青霉素G酰化酶(PGA)在水相体系中酶促合成头孢羟氨苄(cefadroxil)。该实验以温度、p H值、侧链与母核的摩尔比、投酶量、母核浓度和酶的种类等6个因素对头孢羟氨苄合成工艺条件进行优化,转化反应过程中按时取样,利用高效液相色谱仪对母核进行定量分析,追踪母核7-ADCA转化率,直至终止反应。实验结果表明,在温度为20℃、p H6.5、摩尔比1.2:1、投酶量20g、母核浓度13%、采用新A4酶的工艺条件下,母核的转化率可达到99.47%。
[Abstract]:The technological conditions for the synthesis of Cefadroxil by enzyme method were optimized. 7-amino-3-deacetyloxycephalosporic acid (7-amino-3-desacetoxy cephalosporanic acid,7-ADCA) was used as the mother core and p-hydroxyphenylglycine methyl ester (D-hydroxy phenylglycine methyl ester,) was used as the mother core of Cefadroxil (Cefadroxil). D-HPGM) as acyl donor, Cefadroxil (cefadroxil). Was synthesized by penicillin G acylase (PGA) in aqueous system. In this experiment, the synthesis conditions of Cefadroxil were optimized by six factors: temperature, pH value, molar ratio of side chain to mother nucleus, amount of enzyme, concentration of mother nucleus and type of enzyme, and sampling was carried out on time in the process of conversion. The mother nucleus was quantitatively analyzed by high performance liquid chromatography (HPLC) to track the conversion of 7-ADCA in the mother nucleus until the reaction was terminated. The experimental results show that the conversion of mother nucleus can reach 99.47% when the temperature is 20 鈩，
本文编号：2495755
[Abstract]:The technological conditions for the synthesis of Cefadroxil by enzyme method were optimized. 7-amino-3-deacetyloxycephalosporic acid (7-amino-3-desacetoxy cephalosporanic acid,7-ADCA) was used as the mother core and p-hydroxyphenylglycine methyl ester (D-hydroxy phenylglycine methyl ester,) was used as the mother core of Cefadroxil (Cefadroxil). D-HPGM) as acyl donor, Cefadroxil (cefadroxil). Was synthesized by penicillin G acylase (PGA) in aqueous system. In this experiment, the synthesis conditions of Cefadroxil were optimized by six factors: temperature, pH value, molar ratio of side chain to mother nucleus, amount of enzyme, concentration of mother nucleus and type of enzyme, and sampling was carried out on time in the process of conversion. The mother nucleus was quantitatively analyzed by high performance liquid chromatography (HPLC) to track the conversion of 7-ADCA in the mother nucleus until the reaction was terminated. The experimental results show that the conversion of mother nucleus can reach 99.47% when the temperature is 20 鈩，
本文编号：2495755
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