1-(4-羟基苯基)哌嗪氢溴酸盐的合成Synthesis of 1-(4-Hydroxyphenyl) Piperazine Hydrobromide
付晓钟,张珏,袁牧,刘香,张敏,胡伦香
Fu Xiaozhong;Zhang Jue; Yuan Mu; Liu Xiang; Zhang Min; Hu Lunxiang Research Laboratory of Materia Mdia;
摘要(Abstract):
以 β ,β′ 二氯代二乙基胺盐酸盐为起始原料 ,经与对甲氧基苯胺环合反应而得到 1 (4 甲氧苯基 )哌嗪盐酸盐 ,后者经 37%HB与醋酐 (V/V1∶1)回流反应脱去甲基 ,得到 1 (4 羟基苯基 )哌嗪氢溴酸盐 ,将所得产物用红外光谱测定结构 ,通过标准图谱对照 ,证实合成的化合物与目标化合物结构一致。
In order to synthesiye 1 (4 Hydroxyphenyl) piperazine hydrobromide, Bis-2-chloro-ethylamine hydrochloride was used as initial material by cyclizative condensation with p-Aminoanisole to get 1 (4 Methoxyphenyl) piperazine hydrochloride, which was demethylated by heating to reflux in aqueous of 37% HBr and Acetic anhydride (V/V1∶1) to afford the corresponding p-Hydroxy derivative. The synthesized compound was identified with IR spectra. The result showed it was consistent with the proposed structure.
关键词(KeyWords):
脱甲基化;合成工艺;红外光谱
demethylation; synthetical techniques; IR-spectrum
基金项目(Foundation): 贵州省科技基金!资助课题 (计 9610 74)
作者(Authors):
付晓钟,张珏,袁牧,刘香,张敏,胡伦香
Fu Xiaozhong;Zhang Jue; Yuan Mu; Liu Xiang; Zhang Min; Hu Lunxiang Research Laboratory of Materia Mdia;
DOI: 10.19367/j.cnki.1000-2707.2000.01.002
参考文献(References):
- 1RichardA ,Glennon .Conceptsforthedesignof 5-HT1Aserotoninagonistsandantagonists .DrugDerelopmontResearch ,1992 ,2 51- 2 74
- 2PatelUR ,MagidAbou -Ghanbia ,MichaelBWebb ,etal.Polycylicaryl-andhetEroarylpiper azineimidesas 5-HT1Areceptorligands .JMedChem ,1988,31:1382 - 1392
- 3RobertA ,MiltTiteler ,JDMckenney ,etal.Syn thesisandEvaluationofphenglandBenzoylpiper azineaspotenialserotonergicagents.JMedChem ,1986 ,2 9:6 30 - 6 3
- 44David ,L .Structure -ActivityRelationshipsat 5-HT1Areceptor .PharmacologyBiochemistry&Be harior .1991,4 0 :10 4 1- 10 51
- 5 NaimanNA .Stimuluspropertiesofarylpiperazine-NAN - 190 ,apotential 5-HT1Aserotoninan tagonist.DrugDevelopmentResearch ,1989,16 :335- 343
- 6 林寒芬 ,岳 翔 ,陈文杉等 1 乙酰基 4 (4 羟苯基 )哌嗪 (酮康唑 )的合成方法改进 中国医药工业杂志 ,1989,6 2 4 8
- 7 C .B .Pollard ,JoanBChrislie .Derivativesof 1-ArylpiperatinepreparationsandReactionwithE poxides .JChemSoc ,1958,10 32 - 10 4 2
- 8 JCPascal,JullienI ,PinhasH ,etal.Evidenceofaneffectiveantiarrhythmiccompoundbystudyofinvivometabolization .EurJMedChem ,1990 ,2 5:2 911- 2 93
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