| 张宏迪,辛嘉英,孙立瑞,马惠琳,夏春谷.非水相脂肪酶催化氟比洛芬维C酯的合成及条件优化[J].分子催化,2019,33(4):323-330 |
| 非水相脂肪酶催化氟比洛芬维C酯的合成及条件优化 |
| Lipase-catalyzed Synthesis of Flurbiprofen VC Ester |
| 投稿时间：2019-07-10 修订日期：2019-07-23 |
| DOI： |
| 中文关键词: 脂肪酶 氟比洛芬维C酯 非水相反应体系 前药 |
| 英文关键词:lipase flurbiprofen VC ester Non-aqueous reaction system prodrugs |
| 基金项目:黑龙江省应用技术研究与开发计划项目（No.GC13C111）；哈尔滨商业大学研究生创新科研项目（SP17CX006） |
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| 中文摘要: |
| 采用非水相酶催化法合成氟比洛芬维生素C酯，使用高效液相色谱和质谱等方法对产物结构进行了表征.同时构建非水相反应体系，通过研究确定最优合成条件：在10 mL、0.057 mol/L的叔丁醇维生素C溶液中，分别添加2.84 mmol氟比洛芬甲酯，10%的N435脂肪酶（以底物的质量分数计），0.8 g分子筛，在70℃，200 r/min的条件下反应28 h.最优条件下的产物转化率为73.63%. |
| 英文摘要: |
| By using five kinds of organic solvents as reaction medium, the immobilized lipase B from Candida Antarctica (Novozym 435) as the biocatalyst, Lipase-catalyzed synthesis of Flurbiprofen VC ester was studied. Thin-layer chromatogram, high-performance liquid chromatogram and mass spectrum has been used to analyze the structure of the product. The non-aqueous reaction system was established and the reaction condition was optimized. In 10 mL, 0.057 mol/L of vitamin C solution of tert-butanol was added 2.84 mmol flurbiprofen ester, the ratio of enzyme to substrate was 5% (W/W), the mount of molecular sieve was 0.8 g, and the temperature was 70℃, the rotating speed was 200 r/min, After the reaction 28 h, the maximum conversion rate of the product reaches 73.63%. |
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