拉氧頭孢鈉 [cas64953-12-4] 合成路線圖解——原料藥廠家武漢東康源

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1、藥物詳細(xì)合成路線NameMoxalactamdisodium;Latamoxefsodium;S-6059(freeacid);LY-127935;Shiomarin;MoxamChemicalName(6R,7R)-7-[2-(4-Hydroxyphenyl)-3-oxido-3-oxopropionamido]-7-methoxy-3-(1-methyl-1H-tetrazol-5-ylsulfanylmethyl)-8-oxo-5-oxa-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylicaciddisodiumsaltCAS64953

2、-12-4RelatedCAS64952-97-2(freebase)FormulaC20H18N6Na2O9SStructureFormulaWeight564.44486TelE-mail027-8130226718007166089MrYuanchem@whdky.comCompany武漢東康源科技有限公司Activity/MechanismAntibiotics,ANTIINFECTIVETHERAPY,OxacephemsSyn.Route6Route16-(tritylamino)penicillanicacid(i)isconvertedintotheazet

3、idinone(ii),whichistreatedwithp-toluenesulfonicacidtoyieldthetosylate(iii).thechlorinationof(iii)withcl2incarbontetrachlorideaffordsthe4-chloroazetidinone(iv),whichiscondensedwithpropargylalcohol(v)bymeansofagbf4inthftogivethepropargylether(vi)asamixtureofcisandtransisomersthatisseparatedb

4、ychromatography.theacylationof(vi)withphenylacetylchloride(vii)andpyridineaffordstheamide(viii).ListofintermediatesNo.1-allyl-2-bromopyridiniumbromide(v)n-[2-(hydroxymethyl)thieno[3,2-c]pyridin-4-yl]benzamide(vii)(2s)-1-[benzyl(isopropyl)amino]-3-chloro-2-propanol(i)2-[4-([(2s)-3-[benzyl(i

5、sopropyl)amino]-2-hydroxypropyl]oxy)phenyl]acetamide(ii)2,4,5-trifluoro-3-methylbenzoicacid(iii)2,4,5-trifluoro-3-methyl-6-nitrobenzoicacid(iv)2,4,5-trifluoro-3-methyl-6-nitrobenzoylchloride(vi)diethyl2-(2,4,5-trifluoro-3-methyl-6-nitrobenzoyl)malonate(viii)Reference1:narisada,m.;etal.;syn

6、theticstudiesonbeta-lactamantibiotics.part5.asynthesisof7beta-acylamino-3-methyl-1-oxadethia-3-cephem-4-carboxylicacids.heterocycles1977,7,2,839.Reference2:nagata,w.;narisada,m.(shionogi&co.ltd.);arylmalonamido-1-oxadethiacephalosporins.us4180571.Reference3:narisada,m.;nagata,w.(shionogi&c

7、o.ltd.);arylmalonamido-1-oxadethiacephalosporins.de2713370;us4138486.Route2thepartialhydrogenationof(viii)withh2overpd/(caco3)inmethanolgivestheallylether(ix),whichisepoxidizedwithmcpbaindichloromethaneyieldingepoxide(x).epoxidecleavagewiththelithiumsaltof1-me