5-乙酰胺甲基-3-[3-氟-4-(1-哌嗪基苯基)]异噁唑啉的合成  

Synthesis of 5-(Acetamidomethyl)-3-[3-fluoro-4-(1-piperazinyl)phenyl] isoxazoline

作　　者：张智强[1] 刘冰妮[2] 刘默[2] 刘登科[2] 王平保[2] 

机构地区：[1]河南大学药学院,河南开封475001 [2]天津药物研究院,天津300193

出　　处：《精细化工中间体》2009年第3期31-33,共3页Fine Chemical Intermediates

基　　金：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)

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)。The title compound I 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 3,4difluorobenzaldehyde） with a purity of 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 

分 类 号：TQ254.19[化学工程—有机化工]