Oxazolines
    1.
    发明授权
    Oxazolines 失效
    恶唑啉

    公开(公告)号:US4220766A

    公开(公告)日:1980-09-02

    申请号:US868422

    申请日:1978-01-10

    摘要: Useful intermediates for preparing a 1-dethia-1-oxacephalosporin and represented by the following formula: ##STR1## (wherein R is a monovalent group resulting from the elimination of the carbonyl function of an acyl group derived from a carboxylic or carbonic acid;COB is carboxy or protected carboxy; andX is hydrogen or a nucleophilic group)are prepared from the corresponding penicillin 1-oxides of the following formula: ##STR2## (wherein R, COB, and X are as defined above) by heating, if required in the presence of the desulfurizing reagent, or by exchanging the X group with another one under the condition of an appropriate nucleophilic substitution.

    摘要翻译: 用于制备1-脱硫-1-氧杂环孢菌素并由下式表示的有用的中间体:其中R是由消除衍生自羧酸或碳酸的酰基的羰基官能团产生的一价基团; COB 是羧基或被保护的羧基; X是氢或亲核基团)由相应的下式的青霉素1-氧化物制备:如果需要,通过加热,其中R,COB和X如上所定义 在脱硫试剂的存在下,或者通过在适当的亲核取代条件下与另一种X基团交换X基团。

    1-Oxadethiacepham compounds and process for producing said compounds
    2.
    发明授权
    1-Oxadethiacepham compounds and process for producing said compounds 失效
    1-氧杂十八胺化合物及其制备方法

    公开(公告)号:US4366316A

    公开(公告)日:1982-12-28

    申请号:US322662

    申请日:1981-11-18

    IPC分类号: C07D498/04 C07D505/00

    CPC分类号: C07D505/00

    摘要: Intermediates for preparing an antibacterial 1-dethia-1-oxacephalosporins which are represented by the following formula: ##STR1## wherein R is a monovalent group (minus the carbonyl) from an acyl group derived from a carboxylic or carbonic acid;Y.sup.1 is a divalent group of the following formula: ##STR2## wherein COB is carboxy or protected carboxy;X is hydrogen or a nucleophilic group; andZ is a leaving group are prepared from a compound of the following formula: ##STR3## wherein R and Y.sup.1 are as defined above by the action of an acid. The new compounds of this invention shown by the following formula: ##STR4## wherein A is amino or substituted amino;E is hydrogen or methoxy; andY is a divalent group of the following formula: ##STR5## in which COB, X, and Z are as defined above are convertible into other compounds of the same formula by applying conventional methods in .beta.-lactam chemistry.

    摘要翻译: 用于制备由下式表示的抗细菌1-脱氧-1-氧杂头孢菌素的中间体:其中R是衍生自羧酸或碳酸的酰基的一价基团(减去羰基); Y1是下式的二价基团:其中COB是羧基或被保护的羧基; X是氢或亲核基团; 并且Z是离去基团由下式的化合物制备:其中R和Y1如上所定义,通过酸的作用。 本发明的新化合物由下式表示:其中A是氨基或取代的氨基; E是氢或甲氧基; 并且Y是下式的二价基团:其中COB,X和Z如上定义的可通过在β-内酰胺化学中应用常规方法转化为相同式的其它化合物。

    Cephalosporin analogues
    4.
    发明授权
    Cephalosporin analogues 失效
    头孢菌素类似物

    公开(公告)号:US4197402A

    公开(公告)日:1980-04-08

    申请号:US15180

    申请日:1979-02-26

    IPC分类号: C07D505/00 C07D498/00

    CPC分类号: C07D505/00

    摘要: 1-Oxa-cephalosporin analogues of the formula: ##STR1## [wherein X is 3-thienylmalonyl, phenylmalonyl, 4-hydroxyphenylmalonyl, or 2-fluoro-4-hydroxyphenylmalonyl;Y is hydrogen or methoxy; andR is hydrogen, alkali metal, or alkaline earth metal]and the preparation thereof.

    摘要翻译: 具有下式的1-氧杂 - 头孢菌素类似物:其中X是3-噻吩基丙二酰基,苯基丙二酸,4-羟基苯基丙二酸或2-氟-4-羟基苯基丙二酰基; Y是氢或甲氧基; 和R是氢,碱金属或碱土金属]及其制备。

    Haloarylmalonamidooxacephalosporins
    5.
    发明授权
    Haloarylmalonamidooxacephalosporins 失效
    卤代芳基丙酰胺氧基头孢菌素

    公开(公告)号:US4183928A

    公开(公告)日:1980-01-15

    申请号:US900235

    申请日:1978-04-26

    CPC分类号: C07C59/56 C07D505/00

    摘要: Antibacterial haloarylmalonamido-1-dethia-1-oxacephalosporins of the following formula: ##STR1## wherein Ar is ##STR2## (in which Hal and Hal' each is halogen and RO is hydroxy or protected hydroxy);COA and COB each is carboxy or protected carboxy including a pharmaceutically acceptable salt group;and Het is 1-lower alkyl-5-tetrazolyl, 1,3,4-thiadiazol-2-yl or 5-lower alkyl-1,3,4-thiadiazol-2-yl,a pharmaceutical or veterinary composition comprising the said haloarylmalonamido-1-dethia-1-oxacephalosporin and pharmaceutical carrier, and a method for treating or preventing human or veterinary infectious diseases comprising administering an effective amount of the said antibacterial compound.

    摘要翻译: 其中Ar是卤素,Hal和Hal各自为卤素,RO为羟基或被保护的羟基)的抗菌卤代芳基丙二酰胺-1-脱氧-1-氧杂七环素:其中Ar为< ; COA和COB各自为羧基或受保护的羧基,包括药学上可接受的盐基; 和Het是1-低级烷基-5-四唑基,1,3,4-噻二唑-2-基或5-低级烷基-1,3,4-噻二唑-2-基,其包含所述卤代芳基丙二酰胺 -1-脱氢-1-氧杂环孢菌素和药物载体,以及治疗或预防人或兽传感疾病的方法,包括给予有效量的所述抗菌化合物。

    Azetidinone intermediates for cephalosporin analogs
    6.
    发明授权
    Azetidinone intermediates for cephalosporin analogs 失效
    氮杂环丁酮中间体用于头孢菌素类似物

    公开(公告)号:US4592865A

    公开(公告)日:1986-06-03

    申请号:US589670

    申请日:1984-03-13

    摘要: Intermediates of the following formula are useful for the synthesis of 1-oxacephalosporins. Their preparation from penicillins and the transformation process to make 1-oxacephalosporins are disclosed. The compounds are of the formula: ##STR1## wherein A is amino or a selected acylamino;COB is carboxy or a selected protected-carboxy;X is halogen or the group ORin which R is a group represented by following formulas: ##STR2## wherein Nu is a selected nucleophilic group; R.sup.1 is a group of the following formula: ##STR3## in which Hal is halogen or alkylsulfonyloxy and R.sup.2 is alkyl or aryl; andY is hydrogen or methoxy; with the proviso that when R is propargyl or 2-oxopropyl andR.sup.1 is ##STR4## A is in the 3.alpha.-configuration and Y is 3.beta.-hydrogen or A is in the 3.beta.-configuration and Y is 3.alpha.-methoxy.

    摘要翻译: 下列配方的中间体可用于合成1-氧杂七环素。 公开了它们从青霉素的制备和制备1-氧杂七环素的转化过程。 化合物具有下式:其中A是氨基或选择的酰氨基; COB是羧基或选择的保护羧基; X是卤素或基团OR,其中R是由下式表示的基团:CH2CCH,CH2CCNu,CH2CHCH2,&lt; IMAGE&gt;&gt;其中Nu是选择的亲核基团; R1是下式的基团:其中Hal是卤素或烷基磺酰氧基,R2是烷基或芳基的 Y为氢或甲氧基; 条件是当R为炔丙基或2-氧代丙基且R 1为A 3构型时,Y为3个β-氢,或A为3个β-构型,Y为3个α-甲氧基。

    1-Oxadethiacepham compounds
    7.
    发明授权
    1-Oxadethiacepham compounds 失效
    1-氧杂十八胺化合物

    公开(公告)号:US4533730A

    公开(公告)日:1985-08-06

    申请号:US543940

    申请日:1983-10-19

    CPC分类号: C07D505/00

    摘要: Intermediates for preparing an antibacterial 1-dethia-1-oxacephalosporins which are represented by the following formula: ##STR1## wherein R is a monovalent group (minus the carbonyl) from an acyl derived from a carboxylic or carbonic acid;Y.sup.1 is a divalent group of the following formula: ##STR2## wherein COB is carboxy or protected carboxy;X is hydrogen or a nucleophilic group; andZ is a leaving groupare prepared from a compound of the following formula; ##STR3## wherein R and Y.sup.1 are as defined above by the action of an acid. The new compounds of this invention shown by the following formula: ##STR4## wherein A is amino or substituted amino;E is hydrogen or methoxy; andY is a divalent group of the following formula: ##STR5## in which COB, X, and Z are as defined above are convertible into other compounds of the same formula by applying conventional methods in .beta.-lactam chemistry.

    摘要翻译: 用于制备由下式表示的抗菌1-脱氧-1-氧杂头孢菌素的中间体:其中R是衍生自羧酸或碳酸的酰基的一价基团(减去羰基); Y1是下式的二价基团:其中COB是羧基或被保护的羧基; X是氢或亲核基团; 并且Z为离去基团由下式的化合物制备: 其中R和Y1如上所定义,通过酸的作用。 本发明的新化合物由下式表示:其中A是氨基或取代的氨基; E是氢或甲氧基; 并且Y是下式的二价基团:其中COB,X和Z如上定义的 + TR 可通过在β-内酰胺化学中应用常规方法转化为相同式的其它化合物。

    1-Oxadethiacepham compounds
    8.
    发明授权
    1-Oxadethiacepham compounds 失效
    1-氧杂十八胺化合物

    公开(公告)号:US4504659A

    公开(公告)日:1985-03-12

    申请号:US543939

    申请日:1983-10-19

    CPC分类号: C07D505/00

    摘要: Intermediates for preparing an antibacterial 1-dethia-1-oxacephalosporins which are represented by the following formula: ##STR1## wherein R is a monovalent group (minus the carbonyl) from an acyl derived from a carboxylic or carbonic acid;Y.sup.1 is a divalent group of the following formula: ##STR2## wherein COB is carboxy or protected carboxy;X is hydrogen or a nucleophilic group; andZ is a leaving groupare prepared from a compound of the following formula: ##STR3## wherein R and Y.sup.1 are as defined above by the action of an acid.

    摘要翻译: 用于制备由下式表示的抗菌1-脱氧-1-氧杂头孢菌素的中间体:其中R是衍生自羧酸或碳酸的酰基的一价基团(减去羰基); Y1是下式的二价基团:其中COB是羧基或被保护的羧基; X是氢或亲核基团; 并且Z是离去基团由下式的化合物制备:其中R和Y1如上所定义,通过酸的作用。

    1-Oxadethiacepham compounds
    9.
    发明授权
    1-Oxadethiacepham compounds 失效
    1-氧杂十八胺化合物

    公开(公告)号:US4478997A

    公开(公告)日:1984-10-23

    申请号:US543664

    申请日:1983-10-19

    CPC分类号: C07D505/00

    摘要: Intermediates for preparing an antibacterial 1-dethia-1-oxa-cephalosporins which are represented by the following formula: ##STR1## wherein R is a monovalent group (minus the carbonyl) from an acyl derived from a carboxylic or carbonic acid;Y.sup.1 is a divalent group of the following formula: ##STR2## wherein COB is carboxy or protected carboxy;X is hydrogen or a nucleophilic group; andZ is a leaving groupare prepared from a compound of the following formula: ##STR3## wherein R and Y.sup.1 are as defined above by the action of an acid.

    摘要翻译: 用于制备由下式表示的抗菌1-脱氧-1-氧杂 - 头孢菌素的中间体:其中R是衍生自羧酸或碳酸的酰基的一价基团(减去羰基); Y1是下式的二价基团:其中COB是羧基或被保护的羧基; X是氢或亲核基团; 并且Z是离去基团由下式的化合物制备:其中R和Y1如上所定义,通过酸的作用。

    Cyclization to form cephem ring and intermediates therefor
    10.
    发明授权
    Cyclization to form cephem ring and intermediates therefor 失效
    环化形成头孢烯环及其中间体

    公开(公告)号:US4160085A

    公开(公告)日:1979-07-03

    申请号:US856806

    申请日:1977-12-01

    CPC分类号: C07D205/095 Y02P20/55

    摘要: Intermediates represented by the following formulas are useful for synthesizing 3-hydroxy-3-cephem compounds ##STR1## wherein A and B each is a hydrogen or amino substituent; R is a hydrogen or thiol substituent; Hal is a halogen; X is a hydroxy or carboxy protecting group; the broken line between A and R shows that when R and B are hydrogens, and A is a carboxylic acyl, the substituents can be combined to form an azetidinothiazoline bicyclic ring; and the enamine derivatives thereof. One embodiment provides for cyclizing a compound of the formula: ##STR2## wherein A, B, X and Hal are as defined above, which comprises treating the said compound with an acid, base, or solvent if required in the presence of a catalyzer to give a compound represented by following formula ##STR3## In a further embodiment a compound represented by the following formula ##STR4## wherein A, B, R and X are as defined above, is prepared by a process which comprises treating an enamine of a compound represented by following formula ##STR5## wherein A, B, R, X, Hal and broken line are as defined above, with a disubstituted amino containing from 2 to 20 carbon atoms, with the action of an aqueous acid.

    摘要翻译: 由下式表示的中间体可用于合成3-羟基-3-头孢烯化合物,其中A和B各自为氢或氨基取代基; R是氢或硫醇取代基; 卤素是卤素; X是羟基或羧基保护基; A和R之间的虚线表示当R和B为氢时,A为羧酰基时,可以将取代基结合形成氮杂环丁烷异噻唑啉双环; 及其烯胺衍生物。 一个实施方案提供使下式化合物环化:其中A,B,X和Hal如上定义,其包括如果需要,在催化剂存在下用酸,碱或溶剂处理所述化合物, 得到由下式表示的化合物。在另一个实施方案中,由以下通式表示的化合物其中A,B,R和X如上定义的化合物通过包括处理烯胺 其中A,B,R,X,Hal和虚线如上所定义,与含有2-20个碳原子的二取代的氨基酸反应。