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    Process for the preparation of 2,3-epoxyamides
    2.
    发明授权
    Process for the preparation of 2,3-epoxyamides 失效
    2,3-环氧酰胺的制备方法

    公开(公告)号：US4849531A

    公开(公告)日：1989-07-18

    申请号：US043664

    申请日：1987-04-28

    申请人： Dieter Habich ,  Wolfgang Hartwig

    发明人： Dieter Habich ,  Wolfgang Hartwig

    IPC分类号： C07B61/00 ,  B01J31/00 ,  C07D303/48

    CPC分类号： C07D303/48 ,  Y02P20/55

    摘要： A process for the preparation of a 2,3-epoxyamide of the formula ##STR1## in which R.sup.1 represents hydrogen or straight-chain or branched C.sub.1 -C.sub.8 -alkyl, which may be substituted by phenyl or halogen, or represents C.sub.3 -C.sub.7 -cycloalkyl, phenyl, C.sub.1 -C.sub.8 -alkoxycarbonyl, or a group of the formula ##STR2## in which R.sup.4 and R.sup.5 are identical or different and denote hydrogen, phenyl, benzyl, acetyl or C.sub.1 -C.sub.8 -alkyl which is optionally substituted by phenyl or halogen,R.sup.2 represents hydrogen or an amino protecting group andR.sup.3 represents a radical which activates the methylene group,comprising reacting a 2-halogeno-3-hydroxyamide of the formula ##STR3## in which X represents fluorine, chlorine, bromine or iodine,with an alkali metal hydroxide in an inert solvent.

    摘要翻译： 制备式“IMAGE”的2,3-环氧酰胺的方法，其中R 1表示氢或可被苯基或卤素取代的直链或支链C 1 -C 8 - 烷基，或代表C 3 -C 7 - 环烷基，苯基，C 1 -C 8 - 烷氧基羰基或其中R 4和R 5相同或不同并表示氢，苯基，苄基，乙酰基或任选被苯基取代的C 1 -C 8 - 烷基的式 卤素，R 2表示氢或氨基保护基，R 3表示活化亚甲基的基团，包括将其中X表示氟，氯，溴或碘的式“IMAGE”的2-卤代-3-羟基酰胺与 在惰性溶剂中的碱金属氢氧化物。

    Process for the preparation of 7-acylamino-3-hydroxy-cephem-4-carboxylic acids and 7-acylamino-3-hydroxy-1-dethia-1-oxacephem-4-carboxylic acids
    4.
    发明授权
    Process for the preparation of 7-acylamino-3-hydroxy-cephem-4-carboxylic acids and 7-acylamino-3-hydroxy-1-dethia-1-oxacephem-4-carboxylic acids 失效
    制备7-酰基氨基-3-羟基 - 头孢烯-4-羧酸和7-酰基氨基-3-羟基-1-脱硫-1-氧代四氢-4-羧酸的方法

    公开(公告)号：US4616084A

    公开(公告)日：1986-10-07

    申请号：US636470

    申请日：1984-07-31

    申请人： Dieter Habich ,  Wolfgang Hartwig

    发明人： Dieter Habich ,  Wolfgang Hartwig

    IPC分类号： C07C205/42 ,  C07D205/085 ,  C07D501/02 ,  C07D501/59 ,  C07D503/00 ,  C07D505/00 ,  A61K31/545

    CPC分类号： C07D505/00 ,  C07C201/12 ,  C07D205/085 ,  C07D503/00 ,  Y02P20/55

    摘要： A process for the preparation of a 7-acylamino-3-hydroxy-2-cephem-4-carboxylic acid, 7-acylamino-3-hydroxy-1-dethia-1-oxa-3-cephem-4-carboxylic acid or derivative thereof of the general formula ##STR1## in which R.sup.1 is hydrogen or optionally substituted alkyl, alkenyl, alkinyl, aralkyl, aryl, heteroaryl, heteroaralkyl, aryloxyalkyl, heteroaryloxyalkyl, alkoxyalkyl, arylthioalkyl, heteroarylthioalkyl, alkylthioalkyl, alkoxy, aryloxy, alkylthio or arylthio,R.sup.2 is hydrogen, a carboxy-protective group or a pharmaceutically useful ester radical, andX is sulphur or oxygen,which comprises:(a) reacting a compound of the formula ##STR2## with (i) a compound of the formula ##STR3## in which R.sup.2 and X have the abovementioned meaning and Y represents diazo (N.sub.2) or hydrogen (H.sub.2) in an inert solvent in the presence of a Lewis acid or proton acid catalyst, or(ii) a compound of the formulaHX--CH.sub.2 --C.tbd.C--COOR.sup.2 to form an intemediate compound having a triple bond, and hydrating the triple bond, the compounds thus obtained, for Y being hydrogen (H.sub.2)--(in case of Y=diazo (N.sub.2) directly the compounds of general formula (2) are obtained) thereby to produce a compound of the formula ##STR4## (b) reacting such compound with an azide in a solvent in the presence of a base to give a compound of the formula ##STR5## (c) converting said compound to the desired product by (i) irradiation in an inert solvent, or(ii) warming in the presence of a catalyst.The end products are, or can be converted to, known .beta.-lactam antibiotics.

    摘要翻译： 制备7-酰基氨基-3-羟基-2-头孢烯-4-羧酸，7-酰基氨基-3-羟基-1-脱硫-1-氧杂-3-头孢烯-4-羧酸或其衍生物的方法 烯基，炔基，芳烷基，芳基，杂芳基，杂芳烷基，芳氧基烷基，杂芳基氧基烷基，烷氧基烷基，芳硫基烷基，杂芳硫基烷基，烷硫基烷基，烷氧基，芳氧基，烷硫基或芳硫基，其中R 1为氢或任选取代的烷基， R2是氢，羧基保护基或药学上有用的酯基，X是硫或氧，其包括：（a）使式（IMAGE）的化合物与（i）下式化合物 其中R2和X具有上述含义，Y代表重氮（N 2）或氢（H 2）在惰性溶剂中，在路易斯酸或质子酸催化剂存在下，或（ii）式HX-CH2- C 3 C COR CO 2，以形成具有三键的中间体化合物，并且使三键水合，该共聚物 （H）在（Y =重氮（N 2）的情况下直接得到通式（2）的化合物），得到下式的化合物：（b）使此 在碱的存在下在溶剂中与叠氮化合物反应，得到下式的化合物：（c）通过（i）在惰性溶剂中照射将所述化合物转化为所需产物，或（ii）在 存在催化剂。 最终产品是或可以转化为已知的β-内酰胺抗生素。

    Benzazolythio-carbapenem antibiotics
    5.
    发明授权
    Benzazolythio-carbapenem antibiotics 失效
    苯扎硫代碳青霉烯类抗生素

    公开(公告)号：US4840946A

    公开(公告)日：1989-06-20

    申请号：US119752

    申请日：1987-11-12

    申请人： Dieter Habich ,  Wolfgang Hartwig ,  Karl G. Metzger ,  Hans-Joachim Zeiler

    发明人： Dieter Habich ,  Wolfgang Hartwig ,  Karl G. Metzger ,  Hans-Joachim Zeiler

    IPC分类号： C07D477/00 ,  A61K31/397 ,  A61K31/41 ,  A61P31/04 ,  C07D477/20

    CPC分类号： C07D477/20 ,  Y02P20/55

    摘要： Antibiotically active benzazolylthio-carbapenems of the formula ##STR1## in which R.sup.1 represents hydrogen or a hydroxyl-protecting group,R.sup.2 represents hydrogen or a carboxyl-protecting group or an ester radical which can be cleaved off in vivo,R.sup.3 represents hydrogen or C.sub.1 -C.sub.10 -alkyl, C.sub.6 -C.sub.12 -aryl or C.sub.7 -C.sub.14 -aralkyl,R.sup.4 represents hydrogen or represents C.sub.1 -C.sub.10 -alkyl, C.sub.6 -C.sub.12 -aryl or C.sub.7 -C.sub.14 aralkyl, or represents C.sub.1 -C.sub.10 -alkylsulphonyl, C.sub.6 -C.sub.12 -arylsulphonyl or C.sub.7 -C.sub.14 -aralkylsulphonyl, or represents an amino-protecting group, or represents a group of the formula ##STR2## in which R.sup.5, R.sup.6 and R.sup.8 are indentical or different and denote hydrogen, C.sub.1 -C.sub.10 -alkyl, C.sub.6 -C.sub.12 -aryl or C.sub.7 -C.sub.14 -aralkyl,andX represents O, S, NH or NCH.sub.3,or salts thereof.

    摘要翻译： 其中R 1表示氢或羟基保护基，R 2表示氢或羧基保护基或可在体内被切割的酯基的式为“IMAGE”的抗生素活性苯并唑基硫代碳青霉烯类，R3表示氢或C1- C 1 -C 12 - 芳基或C 7 -C 14 - 芳烷基，R 4表示氢或C 1 -C 10 - 烷基，C 6 -C 12 - 芳基或C 7 -C 14芳烷基，或表示C 1 -C 10 - 烷基磺酰基，C 6 -C 12 - 或芳基磺酰基或C 7 -C 14 - 芳烷基磺酰基，或表示氨基保护基，或表示其中R 5，R 6和R 8表示氢，C 1 -C 10 - 烷基，C 6 -C 12 芳基或C 7 -C 14 - 芳烷基，X表示O，S，NH或NCH 3或其盐。

    1-Oxadethiacephalosporin derivatives and antibacterial use thereof
    6.
    发明授权
    1-Oxadethiacephalosporin derivatives and antibacterial use thereof 失效
    1-硫代十八烷基醚衍生物及其抗菌用途

    公开(公告)号：US4631275A

    公开(公告)日：1986-12-23

    申请号：US696275

    申请日：1985-01-30

    申请人： Wolfgang Hartwig ,  Dieter Habich ,  Karl G. Metzger ,  Hans-Joachim Zeiler

    发明人： Wolfgang Hartwig ,  Dieter Habich ,  Karl G. Metzger ,  Hans-Joachim Zeiler

    IPC分类号： A61K31/535 ,  A61P31/04 ,  C07D498/04 ,  C07D505/00 ,  A01N43/90

    CPC分类号： C07D505/00

    摘要： 1-Oxadethiacephalosporin derivatives of the formula ##STR1## in which R.sup.1 denotes hydrogen or halogen,R.sup.2 denotes hydrogen or methoxy,A is a nitrogen-containing positively charged N-containing heterocyclic 5-membered to 7-membered ring which in total can contain up to 4 heteroatoms from the group of N, O and S, to which ring up to two further rings can be fused and which ring may optionally be substituted, the ring being bonded via N,B denotes optionally substituted alkoxy or amino, and the remaining radicals are more or less conventional,which are antibacterially active.

    摘要翻译： 式中，R1表示氢或卤素，R2表示氢或甲氧基的式“IMAGE”的1-硫代十八烷基醚衍生物，A是含氮带正电荷的含氮杂环的5元至7元环，其总共可含有 至4个来自N，O和S的杂原子，其中多达两个另外的环可以被稠合并且哪个环可以被任选取代，该环通过N键合，B表示任选取代的烷氧基或氨基，剩余的 自由基或多或少是常规的，其具有抗菌活性。