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1、司帕沙星的合成工艺研究0fPharmacemics2001.32【9)therewhhrP].WO96/37481,1996一¨一28.(CA1997,126:89377u)_5]DucouxJP,MenezPL,KuneschN.AneHicientandstereose1ec[1vesynthesisofinsectpheromonesbywayolnickel—catalyzed,OrignardreactionSymhsisofgossyplureandpheromonesoleudiapavoniaanddrosophilamelanogaster[J].Te
2、trahedron,1992,48(31):6403—6412.[63黄惟德,胨常庆.多肽台成[M].北京:科学出版杜,1985.47.[7]姜麟忠.催化氢化在有机台成中的应用[M].北京:化学工业出版社,1987.88.SynthesisofAntmypertensiveDrugValsartanJIAQing—Zhong.MAGui—Lin.,LIWen—Zhi,JIANGShao—Haot1.DPp.ofPh…{.g,HetMedicadU州n,2.Dept.ofPha~acoChemistry.Heb~’MedecMUniterstIstajiaxhuang05
3、00171ABSTRACT:Beganwith.一chlorobenzonitrile,4一methyl2cyanobiphenyl(2)wassynthesizedthroughGrignardreaction.Thebrominatedproduct(3)reactedwithL—valinebenzylesterP—toluenesul—fonatetogivethesecondaryamine(4)whichafterreactingwithvalerylchloride,wasdehydrogenatedtogive6followedbythetetrazol
4、eringformationwithNaN3/ZnCl2togivethetitleproduct.KeyWords:valsartan;angiotensinⅡ司帕沙星的合成工艺研究0fPharmacemics2001.32【9)therewhhrP].WO96/37481,1996一¨一28.(CA1997,126:89377u)_5]DucouxJP,MenezPL,KuneschN.AneHicientandstereose1ec[1vesynthesisofinsectpheromonesbywayolnickel—catalyzed,Orignardreac
5、tionSymhsisofgossyplureandpheromonesoleudiapavoniaanddrosophilamelanogaster[J].Tetrahedron,1992,48(31):6403—6412.[63黄惟德,胨常庆.多肽台成[M].北京:科学出版杜,1985.47.[7]姜麟忠.催化氢化在有机台成中的应用[M].北京:化学工业出版社,1987.88.SynthesisofAntmypertensiveDrugValsartanJIAQing—Zhong.MAGui—Lin.,LIWen—Zhi,JIANGShao—Haot1.DPp.of
6、Ph…{.g,HetMedicadU州n,2.Dept.ofPha~acoChemistry.Heb~’MedecMUniterstIstajiaxhuang0500171ABSTRACT:Beganwith.一chlorobenzonitrile,4一methyl2cyanobiphenyl(2)wassynthesizedthroughGrignardreaction.Thebrominatedproduct(3)reactedwithL—valinebenzylesterP—toluenesul—fonatetogivethesecondaryamine(4)wh
7、ichafterreactingwithvalerylchloride,wasdehydrogenatedtogive6followedbythetetrazoleringformationwithNaN3/ZnCl2togivethetitleproduct.KeyWords:valsartan;angiotensinⅡreceptorantagonists;synthesis文章编号;1001—8255(2001)090387一O3司帕沙星的合成工艺研究戚建军,李树有,刘明亮,孙兰英,郭惠元(1.中国医学科学院,中国协和医科大学医药生