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
查看参考文献12篇
文摘
|
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%. |
其他语种文摘
|
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. Thinlayer 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%. |
来源
|
分子催化
,2019,33(4):323-330 【扩展库】
|
关键词
|
脂肪酶
;
氟比洛芬维C酯
;
非水相反应体系
;
前药
|
地址
|
1.
哈尔滨商业大学, 黑龙江普通高校食品科学与工程重点实验室, 黑龙江, 哈尔滨, 150076
2.
中国科学院兰州物理化学研究所, 羰基合成与选择氧化国家重点实验室, 甘肃, 兰州, 730000
|
语种
|
中文 |
文献类型
|
研究性论文 |
ISSN
|
1001-3555 |
学科
|
化学工业 |
基金
|
黑龙江省应用技术研究与开发计划项目
;
哈尔滨商业大学研究生创新科研项目
|
文献收藏号
|
CSCD:6587265
|
参考文献 共
12
共1页
|
1.
Zhao Yi. Design,synthesis and biological evaluation of brain targeting L-ascorbic acid prodrugs of ibuprofen with"lock-in"function.
Europ J Med Chem,2014,82(23):314-323
|
被引
6
次
|
|
|
|
2.
TomaszSiodmiak. High enantioselective novozym 435-catalyzed esterification of (R,S)-flurbiprofen monitored with a chiral stationary phase.
Appl Biochem Biotechnol,2015,175(5):2769-2785
|
被引
1
次
|
|
|
|
3.
Yildiz Hasan. Enantioselective resolution of racemic flurbiprofen methyl ester by lipaseencapsulated mercapto calix [4]arenes capped Fe_3O_4 nanoparticles.
Biopro Biosy Engineer,2017,40(8):1189-1196
|
被引
1
次
|
|
|
|
4.
Mahmoud Sheha. Pharmacokinetic and ulcerogenic studies of naproxen prodrugs designed for specific brain delivery.
Arch Pharm Res,2011,35(3):523-530
|
被引
1
次
|
|
|
|
5.
Xin Jiaying. Synthesis of L-ascorbyl flurbiprofenate by lipase-catalyzed esterification and transesterification reactions.
Bio Med Res Inter,2017:5751262
|
被引
1
次
|
|
|
|
6.
Machhindra Gund A. Gastric-sparing nitric oxide-releasable 'true'prodrugs of aspirin and naproxen.
Bioor & Med Chem Lett,2014,24(24):5587-5592
|
被引
1
次
|
|
|
|
7.
Adam Sikora. Kinetic resolution of a β-adrenolytic drug with the use of lipases as enantioselective biocatalysts.
Med Res J,2018,3(1):38-42
|
被引
2
次
|
|
|
|
8.
Shihui Wang. Enzyme stability and activity in non-aqueous reaction systems: A mini review.
Catalysts,2016,6(2):32
|
被引
2
次
|
|
|
|
9.
徐文婷. 固定化脂肪酶ANL非水催化合成L-抗坏血酸棕榈酸酯.
生物加工过程,2018,16(4):36-39
|
被引
2
次
|
|
|
|
10.
辛嘉英. 脂肪酶催化二次动力学拆分制备高光学纯度(S)-萘普生.
分子催化,2015,29(1):90-95
|
被引
6
次
|
|
|
|
11.
王择. L-抗坏血酸氟比洛芬酯前药的设计、酶催化合成与结构表征.
海峡药学,2010,20(10):213-217
|
被引
1
次
|
|
|
|
12.
刘信宁. L-抗坏血酸洛芬酯非水相酶促合成的动力学与热力学.
生物加工过程,2010,8(6):33-39
|
被引
2
次
|
|
|
|
|