含有4-溴卓酮结构单元的吡唑和异噁唑化合物的合成研究.pdf

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1、第27卷第lO期化学研究与应用Vo1．27．No．102015年1O月ChemicalResearchandApplicationOct．，2015文章编号：1004-1656(2015)10—1581-05Synthesisof4-bromotropone-bearingpyrazoleandisoxazoleLIYang’，CHANGMing·qin，ZHANGHong(CollegeofChemistryandChemicalEngineering，BohaiUniversity，Jinzhou1210

2、00，China)Abstract：Inthisinvestigation，thefirstsynthesisofstructurallynew4-bromotropone-bearingpyrazoleandisoxazolecompounds，namely4-bromo-2-(3-ethoxycarbonyl一1H-pyrazol-5-y1)-7-(methylamino)tropone(4a)and4-bromo-2一(3-ethoxycarbonylisoxazol-5一y1)-7一(methylam

3、ino)tropone(4b)hadbeenachievedingoodyieldsthroughthecondensation-cyclizationreactionofethyl4-(4-bro‘mo-7．(methylamino)-tropone-2-y1)一2，4-dioxobutanoate(6)withhydrazinehydrate(5a)andhydroxylamine(5b)，respectively．Thenewly—synthesizedcompoundscouldbegoodcandi

4、datesforthedevelopmentofcompoundsforuseinmedicinalchemistry．Keywords：4一bromotropone；pyrazole；isoxazole；condensation—eyclization；hydrazinehydrate；hydroxylamine含有4．溴卓酮结构单元的吡唑和异嗯唑化合物的合成研究李阳，常明琴，张红(渤海大学化学化工学院，辽宁锦州121000)摘要：本文通过4一(4-溴-7一(甲氨基)-2-卓酮基)_2，4一二羰基丁酸乙酯(

5、6)和水合肼(5a)及盐酸羟胺(5b)的缩合．环化反应，首次合成了结构新颖的含有4-溴卓酮结构单元的吡唑和异嗯唑化合物，即4溴_2-(3一乙氧羰基-IH-5．吡唑基)-7．(甲氨基)卓酮(4a)和4．溴-2一(3-乙氧羰基5-异嗯唑基)-7．(甲氨基)卓酮(4b)。这两种新合成的化合物可以为开发有用的药物活性先导化合物提供很好的底物。关键词：4．溴卓酮；吡唑；异嗯唑；缩合．环化；水合肼；盐酸羟胺中图分类号：0625文献标志码：AP)rrazoleandisoxazolemoietyareimportantcl

6、as—14-eicosatetraenoicacidsynthase(20-HETE)inhibi—sesofpharmaceuticallyactiveheterocycles，andcon-tors[5]．Apartfromthese，theywerereadilyappliedtostitutesthekeysubunitinmanydrugsubstanceswithdrugdesign，andhadarichchemistrybecauseofabroadrangeofpharmacological

7、activitiessuchastheireasyreductivecleavageandsusceptibilitytoringanti．hyperglycemic⋯，ant[proliferative[2I3]，anti—in．transformations[引．Asaconsequence．extensivesyn．flammatoryandMAO．Binhibitoryactivity[引．Inthistheticeffortshadbeendevotedsurroundingthetworegard

8、，Nakamuraetalreportedthatthepyrazoleandframeworkstodesignandsynthesizenovelandinter-isoxazolederivatives(1)(asshowninFigure1)couldestingpyrazole—-andisoxazole·containingmole--beusedaspotentandselective