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题名: Regioselective synthesis of 3 '-O-caproyl-floxuridine catalyzed by Pseudomonas cepacia lipase
作者: Li, Ning;  Zong, Min-Hua;  Liu, Xiu-Mei;  Ma, Ding
关键词: Pseudomonas cepacia lipase ;  floxuridine ;  3 '-O-caproyl-floxuridine ;  regioselective acylation ;  vinyl caproate
刊名: JOURNAL OF MOLECULAR CATALYSIS B-ENZYMATIC
发表日期: 2007-06-01
DOI: 10.1016/j.molcatb.2007.02.006
卷: 47, 期:1-2, 页:6-12
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology ;  Life Sciences & Biomedicine ;  Physical Sciences
类目[WOS]: Biochemistry & Molecular Biology ;  Chemistry, Physical
研究领域[WOS]: Biochemistry & Molecular Biology ;  Chemistry
英文摘要: 3'-O-Caproyl-floxuridine was prepared successfully through an enzymatic approach. Among the seven commercially available lipases tested, Pseudomonas cepacia lipase displayed the highest activity and regioselectivity towards the acylation of 3'-hydroxyl of floxuridine. Effects of various parameters on the acylation reaction catalyzed by P. cepacia lipase were investigated systematically. The best reaction medium was found to be acetone or acetonitrile. The optimal enzyme dosage, molar ratio of vinyl caproate to floxuridine, and reaction temperature were 40 U, 7.5, and 35 C, respectively. Under the optimal conditions, a substrate conversion of >99% and a regioselectivity of 93.5% could be achieved after a reaction time of 4 h. The half life of P. cepacia lipase was less than 4 batches with acetone or acetonitrile as the solvent. (c) 2007 Elsevier B.V. All rights reserved.
关键词[WOS]: CANDIDA-ANTARCTICA LIPASE ;  ACID ESTER PRODRUGS ;  COLORECTAL-CANCER ;  ORGANIC-SOLVENTS ;  ACYLATION ;  5-FLUORO-2'-DEOXYURIDINE ;  1-BETA-D-ARABINOFURANOSYLCYTOSINE ;  MEDIA ;  IMMOBILIZATION ;  5-FLUOROURACIL
语种: 英语
WOS记录号: WOS:000247432000002
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/140576
Appears in Collections:中国科学院大连化学物理研究所_期刊论文

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作者单位: 1.S China Univ Technol, Lab Appl Biocatalysis, Guangzhou 510640, Peoples R China
2.Chinese Acad Sci, Dalian Inst Chem Phys, State Key Lab Catalysis, Dalian 116023, Peoples R China

Recommended Citation:
Li, Ning,Zong, Min-Hua,Liu, Xiu-Mei,et al. Regioselective synthesis of 3 '-O-caproyl-floxuridine catalyzed by Pseudomonas cepacia lipase[J]. JOURNAL OF MOLECULAR CATALYSIS B-ENZYMATIC,2007,47(1-2):6-12.
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