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    Process for the preparation of reactive penicillanic acid and cephalosporanic acid derivatives
    1.
    发明授权
    Process for the preparation of reactive penicillanic acid and cephalosporanic acid derivatives 失效
    反应性青霉烷酸和头孢烷酸衍生物的制备方法

    公开(公告)号：US4171303A

    公开(公告)日：1979-10-16

    申请号：US812735

    申请日：1977-07-05

    申请人： Magda Huhn ,  Gabor Szabo ,  Gabor Resofszki ,  Eva Somfai

    发明人： Magda Huhn ,  Gabor Szabo ,  Gabor Resofszki ,  Eva Somfai

    IPC分类号： C07D499/00 ,  C07D499/72 ,  C07D501/06 ,  C07D499/04 ,  C07D501/04

    CPC分类号： C07D499/00

    摘要： This invention relates to a process for the preparation of acid amides having the formula (I) or their salts ##STR1## wherein R.sup.1 is hydrogen or an easily removable ester-forming or salt-forming group, preferably a trialkylamino, trialkylsilyl, trichloroethyl, acetoxymethyl, phenacyl, substituted phenacyl, substituted phenyl or benzyl group,R.sup.2 is hydrogen, alkyl group, alkenyl group, alkyl group having an aryl or heterocyclic (preferably furyl or thienyl)-substituent, an aryl group having an alkyl substituent (preferably xylyl), or an aryl, aralkyl or heterocyclic group, (preferably a phenyl, thienyl, or furyl group) which can have one or more substituents,R.sup.3 is hydrogen, or substituted or unsubstituted aryl, alkyl, cycloalkyl or aralkyl group, andX is a group of one of the formulae ##STR2## according to the invention an amine of the formula (II), ##STR3## wherein R.sup.4 is an easily removable ester-forming group, preferably a trialkylamino, trialkylsilyl, trichloroethyl, acetoxymethyl, phenacyl, substituted phenacyl, substituted phenyl or benzyl group, or a salt formed preferably with an alkali metal or a trialkylamine, is acylated with an ester of the formula (III), ##STR4## wherein R.sup.5 is a substituted or unsubstituted aryl, alkyl, cycloalkyl or aralkyl group, and, if desired, substituents R.sup.4 and/or R.sup.5 of the obtained product can be split off, and/or, if desired, the obtained product is converted into its salt or a salt is converted into the free acid.

    摘要翻译： 本发明涉及一种制备具有式（I）的酸酰胺或其盐（I）的方法，其中R 1是氢或易于除去的形成酯或成盐基团，优选三烷基氨基，三烷基甲硅烷基， 三氯乙基，乙酰氧基甲基，苯甲酰甲基，取代的苯甲酰甲基，取代的苯基或苄基，R2是氢，烷基，烯基，具有芳基或杂环（优选呋喃基或噻吩基） - 取代基的烷基，具有烷基取代基的芳基 二甲苯基）或可具有一个或多个取代基的芳基，芳烷基或杂环基（优选苯基，噻吩基或呋喃基），R 3为氢或取代或未取代的芳基，烷基，环烷基或芳烷基，X 是根据本发明的一种式（II）的式（II）的胺，其中R 4是易于除去的成酯基团，优选三烷基氨基，三烷基甲硅烷基，三氯乙基，乙酰氧基 取代的苯甲酰甲基，取代的苯基或苄基，或优选与碱金属或三烷基胺形成的盐，用式（III）的酯，其中R5是取代或 未取代的芳基，烷基，环烷基或芳烷基，并且如果需要，所得产物的取代基R 4和/或R 5可以被分离，和/或如果需要，将得到的产物转化为其盐或盐被转化 进入游离酸。

    Ampicillin derivatives substituted by heterocyclic acyl group
    3.
    发明授权
    Ampicillin derivatives substituted by heterocyclic acyl group 失效
    由杂环酰基取代的氨苄青霉素衍生物

    公开(公告)号：US3953428A

    公开(公告)日：1976-04-27

    申请号：US356120

    申请日：1973-05-01

    申请人： Masuo Murakami ,  Ichiro Isaka ,  Akio Koda ,  Norio Kawahara ,  Teruya Ashiwagi ,  Yukiyasu Murakami ,  Kuniichiro Yano ,  Kohzi Nakano ,  Isao Souzo

    发明人： Masuo Murakami ,  Ichiro Isaka ,  Akio Koda ,  Norio Kawahara ,  Teruya Ashiwagi ,  Yukiyasu Murakami ,  Kuniichiro Yano ,  Kohzi Nakano ,  Isao Souzo

    IPC分类号： A61K31/43 ,  C07D20060101 ,  C07D499/12 ,  C07D499/44 ,  C07D499/68 ,  C07D499/70 ,  C07D499/72

    CPC分类号： C07D499/68

    摘要： The ampicillin derivatives represented by the general formula ##SPC1##Wherein R represents ##SPC2##Wherein R' represents a hydrogen atom, a methyl group, or an ethyl group and A and B each represents a hydrogen atom, a hydroxyl group, a methyl group, a methoxy group, a nitro group, or a halogen atom and further said B may combine with A on the carbon atom at the position to form ##SPC3##Group (where in Z represents --CH=N-- or --CH=CH-- and an R.sup.2 represents a hydrogen atom, a hydroxyl group, a phenyl group, a methyl group, an ethyl group, a methoxy group, an ethoxyl group, a methylthio group, a trifluoromethyl group, a halogen atom, a nitro group, an acetyl group, an acetamido group, a ethoxycarbonyloxy group, or a methylsulfonyl group and further R.sub.2 and ##SPC4##May form a thiazole, isothiazolo, pyrrolo, furo, or benzo fused ring which may be substituted by an oxo group, a methyl group, or an acetyl group) and the dotted line means an arbitrary double bond, ##SPC5##Wherein R.sup.3 and R.sup.4 each represents a hydrogen atom or a methyl group, ##SPC6##Wherein R.sup.5 represents a halogen atom, a methoxy group, a nitro group, or a hydroxyl group and R.sup.6 represents a hydrogen atom, a methoxy group, a halogen atom, a nitro group, or a hydroxyl group, or ##SPC7##Wherein R.sup.7 represents a hydrogen atom or a hydroxyl group, Y represents O or S, and the dotted line means an arbitrary double bond, said substituent group, being bonded to the ampicillin molecule through --CO-- at the 2-position, 3-position, 5-position or 6-position when the oxo group (+0) is at the 4-portion and being bonded to the ampicillin molecule through the --CO-- group at the 2-position, 4-position, or 5-position when the oxy group is at the 6-position, and salts of the ampicillin derivatives.Those compounds are valuable as antibacterial agents.

    摘要翻译： 由通式WHEREIN R表示的氨苄青霉素衍生物代表WHEREIN R'表示氢原子，甲基或乙基，A和B各自表示氢原子，羟基，甲基，甲氧基， 硝基或卤素原子，并且所述B可以与碳原子上的A结合形成基团（其中Z表示-CH = N-或-CH = CH-，R2表示氢原子， 羟基，苯基，甲基，乙基，甲氧基，乙氧基，甲硫基，三氟甲基，卤素原子，硝基，乙酰基，乙酰氨基，乙氧基羰基氧基 或甲基磺酰基，并且还可以是OXO基团，甲基或乙酰基团可以取代的噻唑，异噻唑，吡咯，呋喃，或苯并呋喃环），并且被引导的线表示仲胺双 BOND，其中R 3和R 4各自表示氢原子或甲基 其中，R5表示卤素原子，甲氧基，硝基或羟基，R6表示氢原子，甲氧基，卤素原子，硝基或羟基，或者WHEREIN R7表示 氢原子或羟基，Y表示O或S，虚线表示任意双键，所述取代基通过2-位，3-位，5-位上的-CO-键合到氨苄青霉素分子上 当氧基团（+0）为4-部分时，或6-位，当氧基团为氧基团时，2-位，4-位或5-位通过-CO-基团连接于氨苄青霉素分子 在6位，和氨苄青霉素衍生物的盐。

    Carbenicillin analogues
    4.
    发明授权
    Carbenicillin analogues 失效
    羧苄青霉素类似物

    公开(公告)号：US3926955A

    公开(公告)日：1975-12-16

    申请号：US29179872

    申请日：1972-09-25

    申请人： BEECHAM GROUP LTD

    发明人： BURTON GEORGE ,  DAVIES JOHN SYDNEY ,  HUBBARD ANN FRANCES

    IPC分类号： A23K20/195 ,  A61K31/43 ,  A61P31/04 ,  C07D499/00 ,  C07D499/72 ,  C07D499/46

    CPC分类号： C07D499/00

    摘要： Carbenicillin analogues, non-toxic salts and hydrolyzable monoand di-esters useful in treating infectious diseases caused by Gram-positive and Gram-negative bacteria. The terminal side chain group R is a fully saturated heterocyclic or cycloalkyl radical. The heterocyclic radical has 5, 6 or 7 ring atoms and one or more heteroatoms including oxygen, sulphur, >SO2 or >NR'' wherein R'' is hydrogen, lower alkyl, aryl, aralkyl or aryloxycarbonyl. Cycloalkyl is exemplified by cyclopropyl, cyclopentyl, cyclohexyl or cycloheptyl. Representative penicillins are Alpha carboxycyclopropyl methyl penicillin, Alpha -carboxycyclohexyl methyl penicillin, Alpha -carboxy-2-tetrahydropyranyl methyl penicillin and Alpha -carboxytetrahydrothiophen-1,1-dioxide-3-yl methyl penicillin.

    摘要翻译： 碳青霉素类似物，无毒盐和可水解的单酯和二酯可用于治疗由革兰氏阳性和革兰氏阴性菌引起的感染性疾病。 末端侧链基团R是完全饱和的杂环或环烷基。 杂环基具有5,6或7个环原子和一个或多个包括氧，硫，> SO 2或> NR'的杂原子，其中R'是氢，低级烷基，芳基，芳烷基或芳氧基羰基。 环烷基的实例是环丙基，环戊基，环己基或环庚基。 代表性的青霉素是α-羧基环丙基甲基青霉素，α-羧基环己基甲基青霉素，α-羧基-2-四氢吡喃基甲基青霉素和α-羧基四氢噻吩-1,1-二氧化物-3-基甲基青霉素。

    Process for making esters of 6-(alpha-(carboxy)aryla-cetamido)penicillanic acids
    5.
    发明授权
    Process for making esters of 6-(alpha-(carboxy)aryla-cetamido)penicillanic acids 失效
    制备6-（α-（羧基）芳基 - 鲸蜡基酰氨基）青霉烷酸酯的方法

    公开(公告)号：US3862933A

    公开(公告)日：1975-01-28

    申请号：US27116072

    申请日：1972-07-12

    申请人： PFIZER

    发明人： GOLDMAN IRVING M

    IPC分类号： C07D499/04 ,  C07D499/00 ,  C07D499/12 ,  C07D499/32 ,  C07D499/72 ,  C07F7/18 ,  C07D99/16

    CPC分类号： C07F7/1896 ,  C07D499/00

    摘要： An improved process for making Alpha -(carboxy)arylacetyl derivatives of 6-aminopenicillanic acid esters useful as antibacterial agents and as intermediates for 6-( Alpha (carboxy)arylacetamido)penicillanic acids which comprises acylation of a 6-aminopenicillanic acid ester with a monacid halide of an arylmalonic acid silyl ester in anhydrous reactioninert solvent.

    摘要翻译： 用作6-氨基青霉烷酸酯的α-（羧基）芳基乙酰基衍生物用作抗菌剂和6- [α-（羧基）芳基乙酰胺基]青霉烷酸的中间体的改进方法，其包括将6-氨基青霉烷酸酯与 芳基丙二酸甲硅烷基酯的无水卤化物在无水反应惰性溶剂中。

    Crystalline alkali metal salts of {60 -carboxybenzylpenicillin and process therefor
    7.
    发明授权
    Crystalline alkali metal salts of {60 -carboxybenzylpenicillin and process therefor 失效
    {60-羧基苄基苯酚的晶体碱金属盐及其过程

    公开(公告)号：US3697506A

    公开(公告)日：1972-10-10

    申请号：US3697506D

    申请日：1970-08-07

    申请人： PFIZER

    发明人： BUTLER KENNETH

    IPC分类号： C07D499/00 ,  C07D499/72 ,  C07D99/16

    CPC分类号： C07D499/00

    摘要： Crystalline mono-alkali metal and crystalline di-alkali metal salts of Alpha -carboxybenzylpenicillin and a process for their preparation from crude and amorphous forms of a Alpha carboxybenzylpenicillin and salts thereof, and from aqueous and organic solvent solutions of Alpha -carboxybenzylpenicillin and salts thereof.

    摘要翻译： α-羧基苄基青霉素的结晶一碱金属和结晶二碱金属盐及其由粗α-无定形形式的α-羧基苄基青霉素及其盐及α-羧基苄基青霉素及其盐的水溶液和有机溶剂溶液制备的方法 。