| 5-乙酰胺甲基-3-[3-氟-4-(1-哌嗪基苯基)]异噁唑啉的合成 |
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| 引用本文： | 张智强,刘冰妮,刘默,刘登科,王平保. 5-乙酰胺甲基-3-[3-氟-4-(1-哌嗪基苯基)]异噁唑啉的合成[J]. 精细化工中间体, 2009, 39(3): 31-33 |
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| 作者姓名： | 张智强 刘冰妮 刘默 刘登科 王平保 |
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| 作者单位： | 河南大学,药学院,河南,开封,475001;天津药物研究院,天津,300193 |
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| 基金项目： | 国家科技"重大新药创制"第二批课题资助项目，天津市科技计划资助项目 |
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| 摘 要： | 以3，4-二氟苯甲醛、盐酸羟胺为原料，经缩合反应、氯代反应制得3，4-二氟苯肟氯代物（3）；以烯丙基胺为原料经乙酰化反应制得乙酰烯丙基胺（4）；化合物3与化合物4经环合反应、哌嗪取代反应合成终产物5-乙酰胺甲基-3-[3-氟-4-（1-哌嗪基苯基）]异噁唑啉（呈）。总收率为30．2％，纯度为99．1％（HPLC）。
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| 关 键 词： | 5-乙酰胺甲基-3-[3-氟-4-(1-哌嗪基苯基)]异噁唑啉 3 4-二氟苯甲醛 抗菌药 |
Synthesis of 5-(Acetamidomethyl)-3-[3-fluoro-4-(1-piperazinyl)phenyl] isoxazoline |
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| ZHANG Zhi-qiang,LIU Bing-ni,LIU Mo,LIU Deng-ke,WANG Ping-bao. Synthesis of 5-(Acetamidomethyl)-3-[3-fluoro-4-(1-piperazinyl)phenyl] isoxazoline[J]. Fine Chemical Intermediates, 2009, 39(3): 31-33 |
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| Authors: | ZHANG Zhi-qiang LIU Bing-ni LIU Mo LIU Deng-ke WANG Ping-bao |
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| Affiliation: | 1.College of Pharmacy;Henan University;Kaifeng 475001;China;2.Tianjin Institue of Pharmaceutical Research;Tianjin 300193;China |
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| Abstract: | The title compound 1 is an useful intermediate of isoxazolyl anti-microbial agents.It could be synthesized in several steps.Firstly,condensation of 3,4-Difluorobenzaldehyde and hydroxylamine hydrochloride followed by chlorination with NCS gave chlorinated 3,4-difluorobenzoxime 3.Secondly,reaction of allylamine with acetyl chloride gave acetyl allylamine 4.Finally,title compound 1 was obtained from 3 and 4 in an overal yield of 30.2%(based on 3,4-difluorobenzaldehyde)with a purity of 99.1%(HPLC). |
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| Keywords: | 5-(acetamidomethyl)-3-[3-fluoro-4-(1-piperazinyl)phenyl]isoxazoline 3,4-difluorobenzaldehyde antimicrobial agent |
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