青霉素发酵液直接氧化制备青霉素G亚砜反应条件优化-豆柴文库

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青霉素发酵液直接氧化制备青霉素G亚砜反应条件优化
Abstract:
ThedirectoxidationofpenicillinfermentationbrothtopreparepenicillinGsulfoxidewasstudied.Theeffectsofreactionparameters,includingpH,reactiontime,andoxygenflowrate,ontheyieldofsulfoxidewereinvestigatedandoptimized.Afteroptimization,theyieldofpenicillinGsulfoxidewasincreasedto63.9%,whichwas20.8%higherthanthestartingyield.TheoptimizedreactionconditionscanbeappliedtotheindustrialproductionofpenicillinGsulfoxide.
Introduction:
Penicillinisawidelyusedantibioticintheworld.Thestructureofpenicillinscontainsafour-memberedβ-lactamring,whichisresponsiblefortheirantibacterialactivity.However,theβ-lactamringisalsothemostsusceptiblepartofthemoleculetoenzymaticattack,leadingtothedegradationofpenicillinsandareductionoftheirtherapeuticefficacy.PenicillinGsulfoxideisaderivativeofpenicillinG,whichhasasulfoxidegroupattachedtotheβ-lactamring.Thismodificationhasbeenfoundtoimprovethestabilityandantibacterialactivityofpenicillins.
PenicillinGsulfoxidecanbepreparedbythedirectoxidationofpenicillinGfermentationbrothusingoxygenastheoxidant.Manyfactors,suchaspH,temperature,andoxygenflowrate,canaffecttheyieldofpenicillinGsulfoxide.Inthisstudy,wefocusedontheoptimizationofthereactionconditionstomaximizetheyieldofpenicillinGsulfoxide.
Experimental:
Materials:
PenicillinGfermentationbrothwasobtainedfromapharmaceuticalcompany.Hydrogenperoxide(30%w/w)waspurchasedfromSinopharmChemicalReagentCo.,Ltd.Sodiumhydroxideandhydrochloricacidwereofanalyticalgrade.
Methods:
Step1:Preparationofreactionsolution
ThepenicillinGfermentationbrothwascentrifugedat8000rpmfor15mintoremovetheinsolublecomponents.ThepHofthesupernatantwasadjustedto9.0using0.1Msodiumhydroxide.Hydrogenperoxidewasaddedtothesolutiontoafinalconcentrationof3.0%(v/v).Thereactionsolutionwasthentransferredtoa250mLflask.
Step2:Reaction
Thereactionflaskwasplacedinawaterbathat40°Candanoxygenflowrateof1.0L/minwasmaintainedthroughoutthereaction.Thereactiontimewas6h.ThepHofthesolutionwasmonitoredandmaintainedat9.0byadding0.1Mh