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    Glutaryl 7-ACA derivatives and processes for obtaining them
    3.
    发明授权
    Glutaryl 7-ACA derivatives and processes for obtaining them 失效
    Glutaryl 7-ACA衍生物和获得它们的方法

    公开(公告)号：US6005101A

    公开(公告)日：1999-12-21

    申请号：US17860

    申请日：1998-02-03

    申请人： Loris Sogli ,  Davide Longoni ,  Giovanni Pozzi ,  Enrico Siviero ,  Daniele Mario Terrassan ,  Ermanno Bernasconi ,  Francisco Salto

    发明人： Loris Sogli ,  Davide Longoni ,  Giovanni Pozzi ,  Enrico Siviero ,  Daniele Mario Terrassan ,  Ermanno Bernasconi ,  Francisco Salto

    IPC分类号： C07D501/04 ,  C07D501/00 ,  C07D501/14 ,  C07D501/16 ,  C07D501/20 ,  C07D501/24 ,  C07D501/26 ,  C07D501/28 ,  C07D501/59

    CPC分类号： C07D501/00

    摘要： A compound having the following general formula (I): ##STR1## where R is a hydrogen atom; a linear or branched C.sub.1 -C.sub.4 alkyl group, unsubstituted or substituted by at least a phenyl group or at least a hydrogen atom; a benzyl group substituted by at least a linear or branched C.sub.1 -C.sub.4 alkyl or alkoxy group or a nitro group; a silyl substituted by at least a linear or branched, unsubstituted or substituted C.sub.1 -C.sub.4 alkyl group; n is 0 or 1; and Y is a radical of formula ##STR2## wherein A is H, OH, Cl, CH.sub.2, CH.sub.2 X, where X is F, Cl, Br, I, OH or OR' and R' is COCH.sub.3 or a linear or branched, unsubstituted or substituted C.sub.1 -C.sub.4 alkyl group and - - - represents a single or a double bond, with the proviso that when n=0 and R is H, R' is not a methyl group.

    摘要翻译： 具有以下通式（I）的化合物：其中R是氢原子; 直链或支链C 1 -C 4烷基，未被取代或被至少一个苯基或至少一个氢原子取代; 被至少一个直链或支链的C 1 -C 4烷基或烷氧基或硝基取代的苄基; 由至少一个直链或支链的未取代或取代的C 1 -C 4烷基取代的甲硅烷基; n为0或1; 并且Y是下式的基团，其中A是H，OH，Cl，CH 2，CH 2 X，其中X是F，Cl，Br，I，OH或OR'，R'是COCH 3或直链或支链，未取代或取代的C1 -C4烷基和+ E，未 - - + EE表示单键或双键，条件是当n = 0且R为H时，R'不为甲基。

    Process for the preparation of cephalosporins intermediates
    7.
    发明授权
    Process for the preparation of cephalosporins intermediates 失效
    制备头孢菌素中间体的方法

    公开(公告)号：US5387679A

    公开(公告)日：1995-02-07

    申请号：US988961

    申请日：1993-03-15

    申请人： Loris Sogli ,  Daniele Terrassan ,  Giuseppe Ribaldone

    发明人： Loris Sogli ,  Daniele Terrassan ,  Giuseppe Ribaldone

    IPC分类号： C07D501/00 ,  C07D501/04 ,  C07D501/18 ,  C07D501/26 ,  C07D501/36 ,  A61K31/545

    CPC分类号： C07D501/00 ,  Y02P20/55

    摘要： The present invention relates to a process for preparing a compound of formula (I) ##STR1## wherein R is an heterocyclic group which contains at least one nitrogen atom with or without oxygen or sulphur and R.sup.1 and R.sup.2 are both hydrogen atoms or one of them is an hydrogen atom and the other is an acyl group; the process comprising reacting a compound of formula (II) ##STR2## wherein R.sup.1 and R.sup.2 are each as defined above, and wherein, if necessary, any reactive group is protected by a suitable protective group, or a salt thereof, with a compound of formula (III)R--SH (III)wherein R is as defined above, or a salt thereof, in the presence of an acid and of a compound of formula (IV) ##STR3## wherein each of R.sup.3 and R.sup.4 is a C.sub.1 -C.sub.4 alkyl group or R.sup.3 and R.sup.4 taken together are a C.sub.2 or C.sub.3 alkylene chain and, if necessary, removing the protective groups possibly present.The compounds of formula (I) are useful intermediates in the synthesis of Cefazolin and Cefazedone.

    摘要翻译： PCT No.PCT / EP92 / 01595 Sec。 371日期1993年3月15日 102（e）1993年3月15日PCT提交1992年7月14日PCT公布。 出版物WO93 / 02085 本发明涉及一种制备式（I）化合物的方法，其中含有或不具有氧或硫的至少一个氮原子，且R 1和R 2均为氢原子或其中之一 是氢原子，另一个是酰基; 该方法包括使式（II）化合物其中R 1和R 2各自如上所定义，并且其中如有必要，任何反应性基团被合适的保护基或其盐保护，其中 式（III）化合物其中R如上定义的R-SH（III）或其盐在酸和式（IV）化合物的存在下，其中R 3 并且R 4是C 1 -C 4烷基或R 3和R 4一起是C 2或C 3亚烷基链，并且如果需要，除去可能存在的保护基团。 式（I）化合物是合成头孢唑啉和头孢唑酮的有用中间体。

    Process for the preparation of new intermediates useful in the synthesis of cephalosporins
    10.
    发明授权
    Process for the preparation of new intermediates useful in the synthesis of cephalosporins 失效
    制备可用于合成头孢菌素的新中间体的方法

    公开(公告)号：US5945414A

    公开(公告)日：1999-08-31

    申请号：US982351

    申请日：1997-12-02

    申请人： Loris Sogli ,  Daniele Terrassan ,  Ermanno Bernasconi ,  Francisco Salto

    发明人： Loris Sogli ,  Daniele Terrassan ,  Ermanno Bernasconi ,  Francisco Salto

    IPC分类号： C12P17/14 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/04 ,  C07D501/28 ,  C07D501/36 ,  C12P35/02

    CPC分类号： C12P35/02

    摘要： Cefazolin, cefazedone, cefoperazone, cefamandole, cefatrizine or ceftriaxone is prepared by reacting glutaryl 7-ACA of the formula: ##STR1## with a compound of formula (II):R--SH (II)wherein R is 5-methyl-1,3,4-thiadiazol-2-yl, 1H-1,2,3-triazol-4-yl, 1-methyl-tetrazol-5-yl or1,2,5,6-tetrahydro-2-methyl-5,6-dioxo-1,2,4-triazin-3-yl group, and R.sup.1 and R.sup.2 are both hydrogen and the other is an acyl group, in an aqueous solution in an amount of 3-5 mols per mol of glutaryl 7-ACA to about 90.degree. C. and for a time from about 2 to about 10 hours;optionally recovering the excess of the compound of formula (II), thereby preparing a compound of formula (III) in an aqueous solution: ##STR2## wherein R is as above defined and optionally deacylating said compound of formula (III); andconverting the resulting compound of formula (I) ##STR3## wherein R, R.sup.1 and R.sup.2 are as defined above in the presence of a non-chlorinated solvent into one of said cephalosporins.

    摘要翻译： 通过使下式的戊二酰7 -ACA与式（II）化合物反应来制备头孢唑啉，头孢噻肟，头孢哌酮，头孢匹多，头孢曲松或头孢曲松：R-SH（II）其中R是5-甲基-1,3,4 - 噻二唑-2-基，1H-1,2,3-三唑-4-基，1-甲基 - 四唑-5-基或1,2,5,6-四氢-2-甲基-5,6-二氧代 -1,2,4-三嗪-3-基，R 1和R 2均为氢，另一个为酰基，在每摩尔戊二酰7-ACA至约3-5摩尔量的水溶液中至约 90℃和约2至约10小时的时间; 任选地回收过量的式（II）化合物，从而在水溶液中制备式（III）化合物：其中R如上所定义，并任选地使所述式（III）化合物脱酰; 并将所得的式（I）化合物在非氯化溶剂的存在下转化为所述头孢菌素之一，其中R，R 1和R 2如上定义。