氟替卡松丙酸酯[cas80474-14-2]合成路线图解——原料药厂家东康源

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1、武汉东康源氟替卡松丙酸脂[CAS:80474-14-2]合成路线图解核心提示：NameFluticasonepropionate;FN-25;CCI-18781;Fluspiral;FloventDiskus;Flusonal;FloventDPI;Fluxonal;Flonase;Flunase;Floven.NameFluticasonepropionate;FN-25;CCI-18781;Fluspiral;FloventDiskus;Flusonal;FloventDPI;Fluxonal;Flonase;Flunase;Flovent;Flixotid

2、e;Flutide;Cutivate;FlixonaseChemicalName(6alpha,11beta,16alpha,17alpha)-6,9-Difluoro-11-hydroxy-16-methyl-3-oxo-17-(1-oxopropoxy)androsta-1,4-diene-17-carbothioicacidS-(fluoromethyl)ester　　　　　　6alpha,9-Difluoro-11beta,17-dihydroxy-16alpha-methyl-3-oxoandrosta-1,4-diene-17beta-carboth

3、ioicacidS-(fluoromethyl)ester17-propionateCAS80474-14-2RelatedCASFormulaC25H31F3O5SStructureFormulaWeight500.58202Tel027-8130226718007166089E-mail:chem@whdky.comqq:2847831942Company武汉东康源科技有限公司Activity/MechanismAntiallergy/AntiasthmaticDrugs,AsthmaTherapy,AtopicDermatitis,Agentsfor,Ch

4、ronicObstructivePulmonaryDiseases(COPD),Treatmentof,DERMATOLOGICDRUGS,DrugsforAllergicRhinitis,RESPIRATORYDRUGS,TreatmentofUpperRespiratoryTractDisorders,CorticosteroidsSyn.Route3Route1theoxidationofflumethasone(i)withoxygenandk2co3inmethanolgives6alpha,9alpha-difluoro-11beta,17alpha

5、-dihydroxy-16alpha-methyl-3-oxoandrosta-1,4-diene-17beta-carboxylicacid(ii),whichispartiallyacylatedwithpropionicanhydrideinpyridinetoaffordthecorresponding17alpha-propionyloxyderivative(iii).thereactionof(iii)withdimethylthiocarbamoylchlorideandtriethylamineindichloromethanegivesthe

6、correspondingcarbothioicacid(iv),whichisesterifiedwithbromochloromethaneandsodiumbicarbonateindimethylacetamideyieldingthechloromethylcarbothioateester(v).finally,thiscompoundistreatedwithagfinacetonitrile.ListofintermediatesNo.benzyl(2s)-2-(1,3-dioxo-1,3-dihydro-2h-isoindol-2-yl)-6-

7、hydroxy-6-methylheptanoate(i)benzyl(2s)-6-azido-2-(1,3-dioxo-1,3-dihydro-2h-isoindol-2-yl)-6-methylheptanoate(ii)2-[(3s)-7,7-dimethyl-2-oxoazepanyl]-1h-isoindole-1,3(2h)-dione(iii)(3s)-3-amino-7,7-dimethyl-2-azepanone(iv)tert-butyl(3s)-7,7-dimethyl-2-oxoazepanylcarbamate(v)Reference1

8、:edwards,j.a