第 39 卷第 3 期 | | Vol. 39 No. 3 | 2009 年 6 月 | Jun 2009 |
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所属栏目:医药及中间体
5-乙酰胺甲基-3-[3-氟-4-(1-哌嗪基苯基)]异噁唑啉的合成 |
张智强1,刘冰妮2,刘 默2,刘登科2,王平保2
(1. 河南大学 药学院,河南 开封 475001;2. 天津药物研究院,天津 300193) |
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(1)。总收率为30.2%,纯度为99.1%(HPLC)。 |
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 |
中图分类号:TQ254.19 文献标识码:A 文章编号:1009-9212(2009)02- 0031-03 |
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Synthesis of 5-(Acetamidomethyl)-3-[3-fluoro-4-(1-piperazinyl)phenyl] isoxazoline |
ZHANG Zhi-qiang1,LIU Bing-ni2,LIU Mo2,LIU Deng-ke2,WANG Ping-bao2
(1. College of Pharmacy,Henan University,Kaifeng 475001,China;2. Tianjin Institue of Pharmaceutical Research,Tianjin 300193,China) |
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). |
Key words:5-(acetamidomethyl)-3-[3-fluoro-4-(1-piperazinyl)phenyl]isoxazoline; 3,4-difluorobenzaldehyde;antimicrobial agent |
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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(2009ZX09103-078);天津市科技计划资助项目(09ZCKFSH01300)。
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作者简介:张智强(1984-),男,河南郑州人,硕士研究生,主要从事新药的设计与合成研究。(E-mail:heart51888@yahoo.com.cn)
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收稿日期:2009-05-30
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