头孢唑肟合成工艺的研究

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1、河北科技大学硕士学位论文Abstract(枷甜j【il∞SodiuIIl'oneoftllethirdgenerationc印halosprinsfor两ectionuse，、Ⅳ嬲des“bedindetail’includingitsantibioticmechamsnl，pharmacologicalproperties，clinicale疵ctsandrelatedsyntheticmethods．7rhesymheticprocessofCe斑zoximewasstudied．A盘erinVestigationofas鲥esofsyntheticroutesofo。衔z0

2、虹me，wedeteminedthebeStroute、妇ichwassuitableforscaleproduction．Thesynthesisof7一amino-3-nof．3一cephem一4·c砷o)【)，1icacid(7一√心『CA)w嬲smdied'whichwasanimponantint咖lediateofC硪z踊me．3-Hydroxy一7-beta-phenylac哪!锄inocephem-4一caro)()rlicaciddiphenylmethylester(HCA)、Vassynthesizedfbm3-0Xo-7-p11eIlyl-acetylam

3、inocphem-4一carboxylicaciddiphenylmethylester3一hydr0)【)rc印hemtoluenecomplex)byreductionwithsodiumborohydride．Theyieldofproduct、Ⅳasabout85％．3-Hydro珂一7-beta-phenylacetyl-aminocephem一4一c矧)oxylicdiphenylethyleste①CD)w嬲Synthesized丘omHCAandmethanesulfonylchloride，indichloroethanesolVents．Theyieldofp

4、roductwasbout98．5％．3-hydroxy-7-beta-phenylacetylaminocephem-4一carboxylicwassynthesized疔0mBCD，aluminumtricllloride锄danisole，wtlichdeprotectedn地carbo)【)，lprotecting伊oup．Theyield0fproductwasabout98％．Theproducts0f3一hydroXy-7-b吼a-phenylaCetyla耐nocephem-4一c“boxylicw邪enz)，atichydrolyedtOdeprotectthe

5、aIllino’protecting轳Oup，锄d7一ANCA、Ⅳ嬲obtained．The如eldofproductw嬲about75％．ThetotaJyieldof7-ANCA、抛sabout6l％，ttlepurity0fproduct、Ⅳ邪99．9％．Itw髂appreciatedthatthepr印aration0fceftiz0Ximebyreactionof7-amino一3一no卜3一cephem-4一carboxylicacid(7-ANCA)with2一(2-aminotlliazol4-thiazolyl)-2-【【(Z)meth0．Xy】imino】aC

6、eticaucidS-mercaptobellzotlliazolylester(a嘶vatedeSter)，inthecondition0ftriethyl砌ine．Theyieldofproductw弱about91．8％．11leprodumsofceRizoximesodiumw嬲sy眦hesizedbyce衔zc瞄mesodium2-ethylhexanoate．TheoptiImImCondi：tionswere嬲follows：iniS0prop锄olS0lVem’volumeratioOfiS0prOpyltowaterw勰1O：l，the如eldofceft西)

7、【imesodiumw弱91．8％．Thetotalyieldofceftiz0)【imesodiumw硒about86．8％，tIlepufi哆ofproductw弱99．34％(卸PLC)．ThechenlicalstmcturesOfc硪协融meSodhmhadbeencharacterizedbym％璐0f取锄d1H撇．Theproductqu击时∞cords、析ththe刚加dard0fChin鹤epha删copoeia．K删ordsC印Ⅻospom；CeRiz0)【i