CEPHALOSPORIN DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS

    公开(公告)号:NZ206659A

    公开(公告)日:1986-11-12

    申请号:NZ20665983

    申请日:1983-12-21

    Applicant: HOECHST AG

    Abstract: For the Contracting States : BE, CH, DE, FR, GB, IT, LI, LU, NL, SE 1. Cephem derivatives of the general formula see diagramm : EP0111935,P10,F1 and physiologically acceptable acid addition salts thereof in which R**1 denotes hydrogen, R**2 denotes hydrogen, R**3 denotes C1 -C4 -alkyl optionally substituted by fluorine, A denotes a quinolinium or an isoquinolinium radical, each of which can also be substituted once or twice by C1 -C4 -alkyl and in which the R**3O group is in the syn position. For the Contracting State : AT A process for the preparation of cephem derivatives of the general formula I see diagramm : EP0111935,P11,F1 and physiologically acceptable acid addition salts thereof in which R**1 denotes hydrogen, R**2 denotes hydrogen, R**3 denotes C1 -C4 -alkyl optionally substituted by fluorine, A denotes a quinolinium or an isoquinolinium radical, each of which can also be substituted once or twice by C1 -C4 -alkyl and in which the R**3O group is in the syn position, which comprises a) reacting a compound of the general formula II see diagramm : EP0111935,P11,F2 or salts thereof or a reactive derivative of the compound II in which R**1, R**2 and R**3 have the abovementioned meaning and R**8 denotes an amino group or a protected amino group and R**9 denotes a group which can be replaced by quinoline, isoquinoline or substituted quinolines or isoquinolines corresponding to the radicals A of the formula I, with quinoline, isoquinoline or one of their derivatives, and alpha) splitting off a protective group which is present where appropriate and beta) if necessary, converting the resulting product into a physiologically acceptable acid addition salt, or b) reacting a 7-aminocephen compound of the general formula III see diagramm : EP0111935,P12,F3 or acid addition salts thereof in which R**2 and A have the abovementioned meaning, it also being possible for the amino group to be present in the form of a reactive derivative, with a 2-(2-aminothiazol-4-yl)-2-syn-oximinoacetic acid of the general formula IV see diagramm : EP0111935,P12,F4 in which R**1, R**3 and R**8 have the above meaning, or with an activated derivative of this compound, and alpha) splitting off a protective group which is present where appropriate and beta) if necessary, converting the resulting product into a physiologically acceptable acid addition salt

    POSTOPEK ZA PRIPRAVO CEFEMSKIH SPOJIN

    公开(公告)号:YU45965B

    公开(公告)日:1992-12-21

    申请号:YU76684

    申请日:1984-04-27

    Applicant: HOECHST AG

    Abstract: POSTOPEK ZA PRIPRAVO CEFEMSKIH SPOJIN, s splošno formulo kjer pomeni R tiazolilni ostanek ali 1,2,4-tiadiazolilni ostanek v katerih stoji R3 za vodik in B za amino skupino, in kjer pomeni R1 vodik, R2 metilno skupino, A kinolinijev ostanek , izokinolinijev ostanek metilkinolinijev ostanek ali priridinijev ostanek , ciklopenteno-ali ciklohekseno-piridinijev ostanek ali metilpiridinijev ostanek in v kateri stoji skupina R2-O v sin legi, označen s tem, da spojino s splošno formulo II kjer ima R1 v formuli I navedeni pomen, R7 pomeni skupino, ki se da zamenjati s tisto bazo, ki ustreza ostankom A v formuli I in R8 stoji za vodik ali zaščitno skupino za amino, presnovimo v aprotonskem topilu pri temperaturah med +10 in +80В° C z bazo, ki je osnova v formuli I definiranega ostanka A, in v prisotnosti tri-C1-C4-alkiljodosilana, pri čemer dodamo bazo v stehiometrični množini ali do dvajsetkratnem prebitku, ob tvorbi spojine s splošno formulo III, v kateri imajo R1, R8 in A zgoraj navedeni pomen, in a) v danem primeru prisono zaščitno skupino za amino odcepimo in b) spojino III, kjer pomeni R8 vodik, bodisi kot tako ali v obliki reakcijsko sposobnega derivata presnovimo z 2-sin-oksiminoocetno kislino s splošno formulo IV kjer imata R in R2 navedeni pomen, ali z derivatom te spojine, aktiviranim na karbonilni skupini. Prijava vsebuje še 1 odvisen zahtevek i 1 neovisen zahtevek.

    POSTOPEK ZA PRIPRAVO CEFEMSKIH SPOJIN

    公开(公告)号:YU45966B

    公开(公告)日:1992-12-21

    申请号:YU76784

    申请日:1984-04-27

    Applicant: HOECHST AG

    Abstract: POSTOPEK ZA PRIPRAVO CEFEMSKIH SPOJIN, s splošno formulo I kjer pomeni R tiazolilni ostanek ali 1,2,4-tiadiazolilni ostanek v katerih stojita R3 za vodik ali halogen in B za v danem primeru substituirano amino skupino, in kjer pomeni R1 vodik, R2 nižji alkil, karboksi-nižjialkil, A kinilinijev ali izokinolinijev ostanek ki sta lahko tudi enkrat substituirana z metilom, ali fenantridinijev ostanek ali priridinijev ostanek ki je lahko enkrat ali dvakrat, enako ali različno substituiran z nižjim alkilom, ki je lahko substituiran s sulfo ali metoksi, pri čemer sta lahko 2 alkilni skupini, ki stojita v legi orto, tudi sklenjeni v tri- ali tetrametilenski obroč, v katerem je lahko en obročni ogljikov atom tudi nadomešćen z atomom kisika ali žvepla in v katerem se nadalje lahko nahaja še ena dvojna vez, z metoksi, s halogenom, s fenilom ali s karbamoilom, in v kateri stoji skupina R2O v sin legi, označen s tem, da spojino s splošno formulo II ali njene soli, jer imajo R, R2, R2 pomen, naveden v formuli I, in R7 pomeni skupino, ki se jo da zamenjati s tisto bazo, ki ustreza ostankom A formule I, presnovimo v aprotonskem topilu pri temperaturah med +10 in +80В° C s to bazo v prisotnosti tri-C1-C4-alkiljodosilana, pri čemer dodamo bazo v stehiometrični množini ali do dvajsetkratnem prebitku, in a) v danem primeru prisotno zaščitno skupino odcepimo in b) po potrebi dobljeni produkt prevedemo v fiziološko prenesljivo kislinsko adicijsko sol. Prijava vsebuje še 1 ovisen zahtevek i 1 neovisen zahtevek.

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