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    Cepham compounds
    2.
    发明授权
    Cepham compounds 失效
    Cepham化合物

    公开(公告)号：US4374982A

    公开(公告)日：1983-02-22

    申请号：US290744

    申请日：1981-08-03

    申请人： Robert L. Cundall ,  Derek Walker

    发明人： Robert L. Cundall ,  Derek Walker

    IPC分类号： C07D499/00 ,  C07D501/10 ,  C07D501/18 ,  C07D501/04 ,  A61K31/545

    CPC分类号： C07D499/00

    摘要： Penicillin sulfoxide esters are reacted with an isocyanate to produce the corresponding (substituted)-2-carbamoyloxymethylpenam, the corresponding (substituted)-3-carbamoyloxycepham or the corresponding 3-methylcephem. The 6- or 7-side-chain of these products may be cleaved to give the corresponding 6-amino (penams) or 7-amino (cephams and cephems) compounds, and the latter may be reacylated to produce different 6-acyl-2-carbamoyloxymethyl penams, 7-acyl-3-carbamoyloxy cephams and 7-acyl-3-methylcephems. The substituent groups may be removed from the (substituted)-2-carbamoyloxypenams or the (substituted)-3-carbamoyloxycephams to give the corresponding free 2-carbamoyloxymethylpenams or 3-carbamoyloxycephams, respectively.

    摘要翻译： 将青霉素亚砜酯与异氰酸酯反应以产生相应的（取代的）-2-氨基甲酰氧基甲基氨基钠，相应的（取代的）-3-氨基甲酰氧基头孢烯或相应的3-甲基头孢烯。 这些产物的6-或7-侧链可能被切割，得到相应的6-氨基（半阴离子）或7-氨基（cephams和cephems）化合物，后者可以被再酰化以产生不同的6-酰基-2 - 氨基甲酰氧基甲基半阴离子，7-酰基-3-氨基甲酰氧基Cephams和7-酰基-3-甲基头孢烯。 取代基可以从（取代的）-2-氨基甲酰氧基草酸或（取代的）-3-氨基甲酰氧基头孢中除去，分别得到相应的游离的2-氨基甲酰氧基甲基氨基或3-氨基甲酰氧基头孢。

    Process for preparing a 3-exomethylenecepham sulfoxide from penicillin sulfoxides
    5.
    发明授权
    Process for preparing a 3-exomethylenecepham sulfoxide from penicillin sulfoxides 失效
    从青霉素亚砜制备3-亚甲基头孢烯亚砜的方法

    公开(公告)号：US4075203A

    公开(公告)日：1978-02-21

    申请号：US696674

    申请日：1976-06-16

    申请人： Ta-Sen Chou

    发明人： Ta-Sen Chou

    IPC分类号： C07D205/08 ,  C07D205/09 ,  C07D205/095 ,  C07D409/12 ,  C07D413/12 ,  C07D501/08 ,  C07D501/10 ,  C07D501/02

    CPC分类号： C07D205/095

    摘要： A penicillin sulfoxide ester is reacted with an N-chloro halogenating agent at a temperature of from about 75.degree. C. to about 135.degree. C. and in the presence of an alkylene oxide and calcium oxide to produce a 2-chlorosulfinylazetidin-4-one intermediate. The intermediate, upon separation from the alkylene oxide, calcium oxide, and any conversion products of both the alkylene oxide and calcium oxide, can be treated with stannic chloride to produce a 3-exomethylenecepham sulfoxide.

    摘要翻译： 将青霉素亚砜酯与N-氯卤化剂在约75℃至约135℃的温度下和在环氧烷和氧化钙的存在下反应，得到2-氯亚磺酰基氮杂环丁烷-4-酮 中间。 中间体与烯化氧分离时，氧化钙和氧化烯和氧化钙两者的任何转化产物都可以用氯化锡处理以产生3-异丙基亚甲基亚砜。

    Methods for preparing cephalosporins
    7.
    发明授权
    Methods for preparing cephalosporins 失效
    头孢菌素的制备方法

    公开(公告)号：US4035362A

    公开(公告)日：1977-07-12

    申请号：US672527

    申请日：1976-03-31

    申请人： Paolo Masi ,  Maurizio Foglio ,  Giovanni Franceschi ,  Antonino Suarato ,  Gianfranco Cainelli ,  Federico Arcamone

    发明人： Paolo Masi ,  Maurizio Foglio ,  Giovanni Franceschi ,  Antonino Suarato ,  Gianfranco Cainelli ,  Federico Arcamone

    IPC分类号： C07D205/08 ,  C07D205/095 ,  C07D501/08 ,  C07D501/10 ,  C07D501/20

    CPC分类号： C07D501/08 ,  C07D205/095

    摘要： A process for preparing cephalosporins of the structure: ##STR1## where R is any of hydrogen, C.sub.1 to C.sub.4 alkyl, t-butoxy, benzyloxy, cyano-methyl, thienyl-methyl, furyl-methyl, naphthyl-methyl, phenyl-methyl, phenoxy-methyl, phenoxy-isopropyl, pyridyl-4-thiomethyl and tetrazolyl-1-methyl;R.sub.1 is any of hydroxyl, C.sub.1 to C.sub.4 alkoxy, benzyloxy, p-methoxy- (or nitro-) benzyloxy, benzhydryloxy, triphenylmethoxy, phenacyloxy, p-halophenacyloxy and trichloroethoxy;Z is any of hydrogen, hydroxyl, --O--CO--C.sub.1 -C.sub.4 alkyl, --O--C.sub.1 -C.sub.4 alkyl, --Br, --I, --Cl, --N.sub.3, --NH.sub.2, --O--CO--CH.sub.3, --O--CO--NH.sub.2 and an -S-mononuclear nitrogen heterocyclic ring,By reacting compounds of the structure: ##STR2## IN WHICH R, R.sub.1, and Z are as above defined; R.sub.2 and R.sub.3 are the same or different and represent a C.sub.1 to C.sub.4 alkyl, a mononuclear aryl ring, --CN, a mononuclear heterocyclic ring or the radicals --COR.sub.4, COOR.sub.4, --PO(OR.sub.4).sub.2, --CO--NHR.sub.4 or R.sub.2 and R.sub.3 together may represent: ##STR3## where T represents >CH.sub.2, -N--R.sub.4 ; and R.sub.4 is lower alkyl, a mononuclear aryl ring or a mononuclear heterocyclic ring,Alone or as mixtures with each other in a suitable solvent at a temperature between -100 and +120.degree. C with a strong base to give compounds of formula I that are a mixture of .DELTA..sub.2 and .DELTA..sub.3 cephem-derivatives from which the .DELTA..sub.3 cephem derivatives can be obtained.

    摘要翻译： 一种制备结构式头孢菌素的方法：其中R是氢，C1-C4烷基，叔丁氧基，苄氧基，氰基 - 甲基，噻吩基 - 甲基，呋喃基 - 甲基，萘基 - 甲基，苯基 - 甲基 ，苯氧基甲基，苯氧基 - 异丙基，吡啶基-4-硫代甲基和四唑基-1-甲基; R1是羟基，C1〜C4烷氧基，苄氧基，对甲氧基 - （或硝基）苄氧基，二苯甲氧基，三苯基甲氧基，苯甲酰氧基，对卤代苯氧基和三氯乙氧基中的任一个。 Z是氢，羟基，-O-CO-C 1 -C 4烷基，-O-C 1 -C 4烷基，-Br，-I，-Cl，-N 3，-NH 2，-O-CO-CH 3，-O -CO-NH 2和-S-单核氮杂环，通过反应结构的化合物：其中R，R 1和Z如上所定义;其中R，R 1和Z如上所定义; R2和R3相同或不同，表示C1至C4烷基，单核芳基环，-CN，单核杂环或基团-COR4，COOR4，-PO（OR4）2，-CO-NHR4或R2和 R3一起可以表示：其中T表示> CH 2，-N-R 4; 并且R 4为低级烷基，单核芳基环或单核杂环，单独或混合于适宜溶剂中的温度为-100℃和+120℃之间的强碱，得到式I化合物 可以获得DELTA 2和DELTA 3头孢烯衍生物的混合物，其中可以获得DELTA 3头孢烯衍生物。

    Thioamides of beta-lactam antibiotics
    8.
    发明授权
    Thioamides of beta-lactam antibiotics 失效
    β-内酰胺抗生素的硫胺

    公开(公告)号：US4035354A

    公开(公告)日：1977-07-12

    申请号：US571426

    申请日：1975-04-24

    申请人： Ronald G. Micetich ,  Clinton G. Chin ,  Robert B. Morin

    发明人： Ronald G. Micetich ,  Clinton G. Chin ,  Robert B. Morin

    IPC分类号： C07D499/12 ,  C07D499/00 ,  C07D499/04 ,  C07D499/21 ,  C07D499/44 ,  C07D501/10

    CPC分类号： C07D499/00

    摘要： The invention relates to compounds of the formula: ##STR1## wherein R stands forBenzyl,Phenoxymethyl,4-amino-4-carboxy-1-butyl,R.sup.3 o--, r.sup.3 s--, r.sup.3 r.sup.4 n-- whereinR.sup.3 is loweralkyl, aryl or arylloweralkyl,R.sup.4 is hydrogen or R.sup.3, andR.sup.2 is hydrogen or methoxy, andR.sup.1 is hydrogen or a cleavable radical such as--CH.sub.2 OCH.sub.3, loweralkyl, 2,2,2-trichloroethyl, benzyl, p-nitrobenzyl, benzhydryl, phenacyl or trimethylsilyl. The novel compounds are useful intermediates in the preparation of known penicillin and cephalosporin derivatives.

    摘要翻译： 本发明涉及下式的化合物：其中R代表苄基，苯氧基甲基，4-氨基-4-羧氧基-1-丁基，R3O-，R3S-，R3R4N-，其中R3是低级烷基，芳基或芳基低级烷基，R4 是氢或R3，R2是氢或甲氧基，R1是氢或可分解的基团，例如-CH2OCH3，低级烷基，2,2,2-三氯乙基，苄基，对硝基苄基，二苯甲基，苯甲酰甲基或三甲基甲硅烷基。 该新化合物是制备已知青霉素和头孢菌素衍生物的有用中间体。

    Process for the preparation of cephalosporins from the corresponding azetidinone-thiazoline derivatives
    9.
    发明授权
    Process for the preparation of cephalosporins from the corresponding azetidinone-thiazoline derivatives 失效
    从相应的氮杂环丁酮 - 噻唑啉衍生物制备头孢菌素的方法

    公开(公告)号：US4018776A

    公开(公告)日：1977-04-19

    申请号：US601586

    申请日：1975-08-04

    申请人： Maurizio Foglio ,  Paolo Masi ,  Antonino Suarato ,  Giovanni Franceschi

    发明人： Maurizio Foglio ,  Paolo Masi ,  Antonino Suarato ,  Giovanni Franceschi

    IPC分类号： A61K31/545 ,  C07D20060101 ,  C07D501/04 ,  C07D501/06 ,  C07D501/08 ,  C07D501/10 ,  C07D501/14 ,  C07D501/16 ,  C07D501/20 ,  C07D501/22 ,  C07D501/24 ,  C07D501/28 ,  C07D501/30 ,  C07D501/32 ,  C07D501/34 ,  C07D501/36 ,  C07D501/40 ,  C07D501/42 ,  C07D501/44 ,  C07D501/46 ,  C07D501/60 ,  C07D513/04

    CPC分类号： C07D501/08

    摘要： A process is disclosed for preparing a cephalosporin of structure: ##STR1## where R is selected from the class consisting of hydrogen, alkyl having from 1 to 4 carbon atoms, cyano-methyl, thienyl-methyl, furyl-methyl, naphthyl-methyl, phenyl-methyl, phenoxy-methyl, phenyl-isopropyl, phenoxy-isopropyl, pyridyl-4-thiomethyl, tetrazolyl-1-methyl;R.sup.1 is selected from the class consisting of hydroxy, alkoxy having from 1 to 4 carbon atoms, trichloroethoxy, benzyloxy, p-methoxy-benzyloxy, p-nitrobenzyloxy, benzhydryloxy, triphenylmethoxy, phenacyloxy, p-halophenacyloxy; andZ is selected from the class consisting of hydrogen, hydroxy, --O--Alkyl, --O--CO--Alkyl, --Br, --I, --NH.sub.2, --O--COCH.sub.3, --O--CO--NH.sub.2, and an --S-mononuclear nitrogen heterocyclic ring,Wherein a compound of structure: ##STR2## where R, R.sup.1 and Z have the above meanings, is reacted with iodine in a suitable aqueous solvent at a temperature between 5.degree. and 80.degree. C in the presence of an oxide of a heavy metal or with a free radical initiator under the influence of light or heat, to give a compound of structure: ##STR3## in which R, R.sup.1 and Z have the above meanings, AND THE SAID INTERMEDIATE (II) is reacted in a suitable solvent with a compound selected from the class consisting of inorganic and organic bases to finally give the desired compound (III) which is then isolated and purified in per se known manner.

    摘要翻译： 公开了一种制备头孢菌素的方法，其结构如下：其中R选自氢，具有1至4个碳原子的烷基，氰基 - 甲基，噻吩基 - 甲基，呋喃基 - 甲基，萘基 - 甲基，苯基 - 甲基，苯氧基 - 甲基，苯基 - 异丙基，苯氧基 - 异丙基，吡啶基-4-硫代甲基，四唑基-1-甲基; R1选自羟基，具有1至4个碳原子的烷氧基，三氯乙氧基，苄氧基，对甲氧基 - 苄氧基，对硝基苄氧基，二苯甲氧基，三苯甲氧基，苯甲酰氧基，对卤代苯甲酰氧基; 并且Z选自氢，羟基，-O-烷基，-O-CO-烷基，-Br，-I，-NH2，-O-COCH3，-O-CO-NH2和-S - 单核氮杂环，其中R，R 1和Z具有上述含义的化合物：其中R，R 1和Z具有上述含义，在合适的水性溶剂中，在5℃至80℃的温度下， 重金属的氧化物或在光或热的影响下的自由基引发剂，得到结构式为的化合物：其中R，R 1和Z具有上述含义，并且所述中间体（II） ）在合适的溶剂中与选自无机和有机碱的化合物反应，最终得到所需的化合物（III），然后以本身已知的方式分离和纯化。

    Process for the rearrangement of penicillins to cephalosporins and intermediate compounds thereof
    10.
    发明授权
    Process for the rearrangement of penicillins to cephalosporins and intermediate compounds thereof 失效
    将青霉素重排为头孢菌素及其中间体化合物的方法

    公开(公告)号：US4010156A

    公开(公告)日：1977-03-01

    申请号：US602623

    申请日：1975-08-07

    申请人： Abraham Nudelman ,  Ronald J. McCaully

    发明人： Abraham Nudelman ,  Ronald J. McCaully

    IPC分类号： C07D213/20 ,  C07D215/10 ,  C07D501/10

    CPC分类号： C07D215/10 ,  C07D213/20

    摘要： Penicillin sulfoxides are converted to 3-halo-3-methyl-cepham-4-carboxylic acid esters and amides or the corresponding cephem derivatives by heating the penicillin sulfoxide precursor in a polyhaloalkane solvent to a temperature between 50.degree. to about 150.degree. C. in the presence of an equimolar amount of a neutral or basic catalyst, respectively. The catalysts employed are bases such as pyridine, picoline, lutidine, quinoline, isoquinoline, dimethylaniline or a quaternary ammonium salt. The 3-halo-cepham intermediates produced with a quaternary ammonium catalyst are dehydrohalogenated to afford known cephem derivatives or converted to the free 4-carboxylic acid and the alkali metal, alkaline earth metal or ammonium salts thereof to afford novel antibacterial agents.

    摘要翻译： 将青霉素亚砜转化为3-卤代-3-甲基 - 头孢烯-4-羧酸酯和酰胺或相应的头孢烯衍生物，通过将多卤烷溶剂中的青霉素亚砜前体加热至50℃至约150℃的温度 分别存在等摩尔量的中性或碱性催化剂。 所使用的催化剂是诸如吡啶，甲基吡啶，二甲基吡啶，喹啉，异喹啉，二甲基苯胺或季铵盐的碱。 用季铵催化剂制备的3-卤代 - 头孢烯中间体被脱卤化氢以提供已知的头孢烯衍生物或转化为游离的4-羧酸及其碱金属，碱土金属或铵盐，得到新的抗菌剂。