首页> 外国专利> DERIVATIVES OF 3-AMMONIOPROPENYLCEPHEM-4-CARBOXYLATE WITH ANTIBACTERIAL ACTIVITY, DERIVATIVE OF 3-IODOPROPENYLCEPHEM AS AN INTERMEDIATE PRODUCT FOR THE SYNTHESIS OF DERIVATIVES OF 3-AMMONIOPROPENYLCEPHEM-4-CARBOXYLATE, 2-(5-TRITYLAMINO-1,2,4-THIADIAZOL-3-YL)-(Z)-2-FLUOROMETHOXYIMINOACETIC ACID AS AN INTERMEDIATE COMPOUND FOR T

DERIVATIVES OF 3-AMMONIOPROPENYLCEPHEM-4-CARBOXYLATE WITH ANTIBACTERIAL ACTIVITY, DERIVATIVE OF 3-IODOPROPENYLCEPHEM AS AN INTERMEDIATE PRODUCT FOR THE SYNTHESIS OF DERIVATIVES OF 3-AMMONIOPROPENYLCEPHEM-4-CARBOXYLATE, 2-(5-TRITYLAMINO-1,2,4-THIADIAZOL-3-YL)-(Z)-2-FLUOROMETHOXYIMINOACETIC ACID AS AN INTERMEDIATE COMPOUND FOR T

机译:具有抗菌活性的3-氨丙基戊基乙炔-4-羧酸酯的衍生物,3-碘戊戊基乙炔的衍生物是合成3-氨戊基戊炔基-4-羧酸的衍生物的中间体,2-(5-三氟叠氮基1,2-4-噻吩基-3-YL)-(Z)-2-氟代乙氧基亚氨基乙酸作为T的中间体

摘要

The invention relates to cephem derivatives, in particular the compounds of the general f-ly I and f-II and III: K-tgC-C (0) - | -f (I) HJiJUb-o-CM, oL-, 1 J-fn. sn-si . .o c-o A- 9 (CHJfD4JCW |) -CHI-C (0) -NH; fCtolNHj, HOH.C, - (Sn,) ,,) - with ((H-ni; -fCMjIj-cf-njfCMjj-ooj-trH. ™ .XS, -OH -KfCHj), - Cf-.H ) (OHJ-C (0) NM ;; - (TJ i Г rf / Urt, ПГ V / I Г CHj-ttOJ-MH, / ° CHtc (omHt CH, OH CM, CH. У; - CMtC (-o CH (CH, -NfCMjVCH.-CfO (CH,), -C (-H) (OH); C (0) NH, (B) (Wl-HH-Cc-cp, .. MHT: r CH CH-cH, J. 5-0-CH1f0j-Nv: c (0) OI N-- C-C | 0) -OH (“) .ocMtf l-Nl CHjJj-CI -CfOI-W; - AND-C #) WH,; CHfCHjl-CJO-MM, {HI Compounds of f-ly I have antibacterial activity that can be used in medicine, compound of f-ly II can be used as an intermediate for the synthesis of 3-ammonium derivatives - ropenylcepheme-4-carboxylate, and compound f-ly III can be used to synthesize p-metox benzyl-7- / - 2- (5-tritylamino-1,2,4-thiadiazol-3-yl) - (Z) - (2-fluoromethoxyiminoacetamido) -3- (Е) - {3-iodo-1 -propen-1-yl} 3-cephemcarboxylate The aim is to create new intermediates for more active cephalosporin antibiotics Synthesis of f-III compound is carried out by hydrolysis of its ethyl ester in the presence of alkali while boiling in an aqueous-ethanolic medium. Synthesis of compound f-ly II is carried out by iodination of the corresponding chloride with NaJ in acetone medium, followed by conversion of the obtained iodide into the target product f-ly I, by treating with an appropriate ammonium compound (containing radical A). New Ј
机译:本发明涉及头孢烯衍生物,特别是通式f-ly I和f-II以及III的化合物:K-tgC-C(0)-|。 -f(I)HJiUb-o-CM,oL-,1 J-fn。 sn-si。 .o c-o A-9(CHJfD4JCW |)-CHI-C(0)-NH; fCtolNHj,HOH.C,-(Sn,),,)-具有((H-ni; -fCMjIj-cf-njfCMjj-ooj-trH。™.XS,-OH -KfCHj),-Cf-.H)( OHJ-C(0)NM ;;--(TJ i rf / Urt,ПГV / IГCHj-ttOJ-MH,/°CHtc(omHt CH,OH CM,CH.У;-CMtC(-o CH( CH,-NfCM i VCH -CfO(CH,),-C(-H)(OH); C(0)NH,(B)(W1-HH-Cc-cp,.. MHT:r CH CH-cH, J. 5-0-CH1f0j-Nv:c(0)ON N-- CC | 0)-OH(“).ocMtf l-Nl CHjJj-CI -CfOI-W;-AND-C#)WH ,; CHfCHjl -CJO-MM,{HI f-ly I的化合物具有抗菌活性,可用于医学,f-ly II的化合物可用作合成3-铵衍生物-ropenylcepheme-4-羧酸盐的中间体,化合物f-ly III可用于合成对甲氧基苄基-7- /-2-(5-三苯甲基氨基-1,2,4-噻二唑-3-基)-(Z)-(2-氟甲氧基亚氨基乙酰氨基)- 3-(Е)-{3-碘-1-丙-1-基} 3-头孢羧酸酯目的是为更具活性的头孢菌素抗生素创造新的中间体。f-III化合物的合成是通过将其乙酯水解一个的存在lkali,同时在乙醇水溶液中沸腾。化合物f-ly II的合成是通过在丙酮介质中用NaJ碘化相应的氯化物,然后通过用适当的铵化合物(含基团A)处理将获得的碘化物转化为目标产物f-ly I来进行的。 。新Ј

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