| 吕海军,康彩红,刘磊,于奕峰,陈爱兵,刘红厚,刘欢,张焕鹏,康笑.化学通报,2017,80(9):858-862. |
| 酶法合成头孢丙烯工艺研究 |
| Study on the enzymaticSsynthesis of cefprozil |
| 投稿时间：2017-03-01 修订日期：2017-04-14 |
| DOI： |
| 中文关键词: 头孢丙烯 青霉素G酰化酶 合成水解比 收率 |
| 英文关键词:Cefprozil, Penicillin G acylase, Synthetic hydrolysis ratio, Yield |
| 基金项目:(B2014208121),河北科技大学大学生创新创业训练计划项目(201510082017),河北科技大学五大平台开放基金 (2015PT37) |
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| 中文摘要: |
| 通过对青霉素G酰化酶(PGA)催化合成头孢丙烯的工艺条件进行优化,得到相关实验数据,为头孢丙烯绿色生产技术的推行打下基础。该优化工艺是以7-氨基-3-[(Z)-烯丙基-1-基] -3-头孢环-4-羧酸(7-APCA)为底物,D-对羟苯甘氨酸甲酯(D-HPGME)为酰基供体,水作溶剂,固定化青霉素G酰化酶为催化剂合成头孢丙烯。筛选合适的催化剂酶活并分别采用氨基和环氧载体固载,考察反应pH值、温度、投酶量、投料比、底物浓度等多个因素对酶法合成头孢丙烯的影响。结果显示：以氨基载体合成头孢丙烯的较适宜条件为pH=6.0～6.5；温度25℃；投酶量/7-APCA(质量比)=1.2:1,D-HPGME:7-APCA=1.2:1；底物浓度500mmol/L。此工艺条件下合成水解比S/H可达5以上,收率为63-72%。以环氧载体合成头孢丙烯的较适宜合成条件为温度pH=6.0～6.5；25℃；投酶量/7-APCA(质量比)=1.3:1,投料比HPGM:7-APCA=1.1:1；底物浓度500mmol/L。此工艺条件下合成水解比S/H可达8以上,收率为76-80%。 |
| 英文摘要: |
| The optimization experiments of synthesizing cefprozil with penicillin G acylase as catalyst were successfully achieved, which can lay the foundation of the green production technology of cefprozil. The enzymatic synthesis of cefprozil was operated with 7-amino-3-cephem-4-carboxylicacid (7-APCA) as the mother nucleus, D-hydroxyl methyl phenyl glycine (D-HPGME) as acyl donor, water as solvent and immobilized penicillin Gacylase as enzymatic catalyst. The influence factors of enzymaticSsynthesis of cefprozil such as pH, temperature, enzyme dosage, and feed ratio substrate concentration were researched under the condition of appropriate enzyme activity with amino carrier and epoxy carrier. The result revealed that, more than 5 of hydrolysis ratio and yield of 63-75% were achieved using amino carrier with pH value of 6.0 ~ 6.5, the temperature of 25℃, the mass ratio of enzyme:7-APCA (1.2:1) and HPGM:7-APCA (1.2:1), and substrate concentration of 500mmol/L. Under similar conditions, when pH value is 6.0 ~ 6.5, the temperature is 25℃, the mass ratio enzyme and 7-APCA is 1.3:1 and HPGM: 7-APCA = 1.1:1, the substrate concentration is 500mmol/L, more than 8 of synthetic hydrolysis ratio and the yield of 76-80% were obtained using epoxy carrier. |
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