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1、藥物詳細(xì)合成路線NameAminoglutethimide;AG-1;Orimeten;CytadrenChemicalName3-(4-Aminophenyl)-3-ethyl-2,6-piperidinedioneCAS125-84-8RelatedCASFormulaC13H16N2O2StructureFormulaWeight232.28467TelE-mail027-8130226718007166089MrYuanchem@whdky.comCompany武漢東康源科技有限公司Activity/MechanismAdrenocorticalDysf
2、unctionTherapy,BreastCancerTherapy,CushingsSyndrome,Agentsfor,ENDOCRINEDRUGS,OncolyticDrugs,ProstateCancerTherapy,Antiglucocorticoids,AromataseInhibitorsSyn.Route1Route1animprovedprocedureforthelarge-scalepreparationof(r)-aminoglutethimidehasbeenreported.nucleophilicsubstitutionof1-c
3、hloro-4-nitrobenzene(i)withmethylcyanoacetateaffordedthe(nitrophenyl)cyanoacetate(ii),whichwasalkylatedwithdiethylsulfateinthepresenceofet3n,yielding(iii).hydrolysisanddecarboxylationofthecyanoester(iii)bymeansofk2co3inaqueousmeohprovidedthearylbutyronitrile(iv).subsequentmichaeladdi
4、tionwithmethylacrylategaveadduct(v).thiswashydrolyzedtothecyanoacid(vi),whichwasfurtherresolvedwith(-)-cinchonidine,yieldingthedesired(r)-enantiomer(vii).acid-catalyzedcyclizationof(vii)inboilingtoluenegeneratedtheglutarimidederivative(viii).thenitrogroupof(viii)wasfinallyreducedtoth
5、etitleaminoderivativebyhydrogenationoverpd/c.ListofintermediatesNo.(4s,7r,8s,9s,16s)-8-hydroxy-5,5,7,9,13-pentamethyl-16-[(e)-1-methyl-2-(2-methyl-1,3-thiazol-4-yl)ethenyl]-4-[(triethylsilyl)oxy]oxa-13-cyclohexadecene-2,6-dione(i)1-methyl-2-oxo-1,2-dihydro-4-pyridinecarbaldehyde2-(2-
6、phenyl-1h-indol-3-yl)-1-ethanamine;2-(2-phenyl-1h-indol-3-yl)ethylamine(1as,8r,9as)-3-(acetoxy)-7-(benzyloxy)-5-[[(benzyloxy)methoxy]methyl]-8-(hydroxymethyl)-1-[(4-methylphenyl)sulfonyl]-1,1a,2,3,8,9a-hexahydro-9h-azireno[2,3-c][1]benzazocin-9-one(ii)(1as,8r,9as)-7-(benzyloxy)-5-[[(
7、benzyloxy)methoxy]methyl]-3-hydroxy-8-(hydroxymethyl)-1-[(4-methylphenyl)sulfonyl]-1,1a,2,3,8,9a-hexahydro-9h-azireno[2,3-c][1]benzazocin-9-one(iii)(8r,9s,10s,12s)-6-(benzyloxy)-4-[[(benzyloxy)methoxy]methyl]-8-(hydroxymethyl)-11-[(4-methylphenyl)sulfonyl]-14-oxa-1,11-diazatetracyclo
8、[7.4.1.0(2,7
