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120 条记录 (耗时 0.028 秒)

    INTERMEDIATES IN THE SYNTHESIS OF C3-SUBSTITUTED CEPHALOSPORINS
    21.
    发明申请
    INTERMEDIATES IN THE SYNTHESIS OF C3-SUBSTITUTED CEPHALOSPORINS 有权

    公开(公告)号：US20210261571A1

    公开(公告)日：2021-08-26

    申请号：US17255371

    申请日：2019-07-02

    申请人： Norbrook Laboratories Limited, Carnbane

    发明人： Karolina MADELA

    IPC分类号： C07D501/10 ,  C07D307/16

    摘要： Disclosed herein are novel and inventive methods for preparing intermediates in the synthesis of C3-substituted cephalosporins. One preferred C3-substituted cephalosporin of clinical interest is Cefovecin. Accordingly, the present invention provides for methods of preparing reactive halogen intermediates for use in the synthesis of C3-substituted cephalosporins, such as Cefovecin. In the case of Cefovecin the reactive intermediates are of the formula:

    Method for the preparation of 2-chloro sulfinyl azetidinones
    23.
    发明授权
    Method for the preparation of 2-chloro sulfinyl azetidinones 失效
    2-氯亚磺酰基氮杂环丁酮的制备方法

    公开(公告)号：US5604222A

    公开(公告)日：1997-02-18

    申请号：US173757

    申请日：1993-12-27

    申请人： Niranjan L. Gupta ,  Ramanathan Sankaran ,  Sakina Sitabkhan

    发明人： Niranjan L. Gupta ,  Ramanathan Sankaran ,  Sakina Sitabkhan

    IPC分类号： C07D205/095 ,  C07D409/12 ,  C07D499/04 ,  C07D501/00 ,  C07D501/10 ,  C07D501/14

    CPC分类号： C07D409/12 ,  C07D205/095 ,  C07D501/00 ,  Y02P20/55

    摘要： An improved method for the preparation of 2-chloro sulfinyl azetidin-4-one of the formula: ##STR1## wherein R is: hydrogen; C.sub.1 -C.sub.3 alkyl; halomethyl; cyanomethyl; phenyl; substituted phenyl; phenoxy, benzyloxy- or substituted benzyl; a group of the formula R.sub.2 --O--wherein R.sub.2 is t-butyl, 2,2,2-trichloroethyl, benzyl or substituted benzyl; a group of the formula R.sub.3 --(O).sub.n --CH.sub.2 wherein R.sub.3 is phenyl or substituted phenyl. The 2-chlorosulfinylazetidin-4-one is prepared by reacting a penicillin sulfoxide ester of the general formula ##STR2## wherein R and R.sub.1 have the meanings defined above with an N-chloro halogenating agent in an inert organic solvent. The reaction is carried out in the presence of an acid scavenging amount of a phosphate or hydrogen phosphate of an alkali metal, alkaline earth metal, ammonium, quaternary ammonium or mixtures thereof. These compounds find application as intermediates in the production of cefaclor which are powerful anti-bacterial compounds.

    摘要翻译： 用于制备下式的2-氯亚磺酰基氮杂环丁烷-4-酮的改进方法：; 氰甲基 苯基; 取代的苯基; 苯氧基，苄氧基或取代的苄基; 式R2-O-的基团，其中R2是叔丁基，2,2,2-三氯乙基，苄基或取代的苄基; 式R 3 - （O）n -CH 2的基团，其中R 3是苯基或取代的苯基。 2-氯亚磺酰基氮杂环丁烷-4-酮的制备方法是将惰性有机溶剂中通式为“IMAGE”的青霉素亚砜酯，其中R和R 1具有上述定义与N-氯卤化剂反应。 该反应在酸清除量的碱金属，碱土金属，铵，季铵或其混合物的磷酸盐或磷酸氢盐存在下进行。 这些化合物可用作生产头孢克洛的中间体，它们是强大的抗菌化合物。

    Method for the preparation of .DELTA..sup.3 -7-substituted amino desacetoxy cephalosporanic acid
    24.
    发明授权
    Method for the preparation of .DELTA..sup.3 -7-substituted amino desacetoxy cephalosporanic acid 失效
    制备δ3-7取代氨基脱乙酰氧基头孢菌酸的方法

    公开(公告)号：US5302713A

    公开(公告)日：1994-04-12

    申请号：US861232

    申请日：1992-03-31

    申请人： Jinun B. Yeh ,  Lain-Tze Lee ,  Mei-Hueih Chen

    发明人： Jinun B. Yeh ,  Lain-Tze Lee ,  Mei-Hueih Chen

    IPC分类号： C07D501/00 ,  C07D501/22 ,  C07D501/10

    CPC分类号： C07D501/00

    摘要： A method for synthesizing .DELTA..sup.3 -7-substituted amino desacetoxy cephalosporanic acid from a penicillin sulfoxide or its alkylsilylated ester derivative is provided. According to the method, penicillin sulfoxide is heated in the presence of an organic ammonium salt catalyst and a copolymer composed of dimethylsilane and urea units until formation of the cephalosporanic acid occurs by ring expansion reaction. The copolymer functions both as a dehydrating agent for removing the water by-product generated from the reaction as well as an esterifying agent for converting penicillin sulfoxide into its dimethylsilyl ester derivative. The method of the invention produces high yields of the cephalosporanic acid and avoids the need for excess dimethylsilyating agents.

    摘要翻译： 提供了从青霉素亚砜或其烷基硅烷化酯衍生物合成DELTA 3-7-取代氨基脱乙酰氧基头孢菌酸的方法。 根据该方法，在有机铵盐催化剂和由二甲基硅烷和尿素单元组成的共聚物存在下，加热青霉素亚砜，直到通过环扩展反应发生形成头孢菌酸。 该共聚物既用作去除由反应产生的水副产物的脱水剂也用作将青霉素亚砜转化为其二甲基甲硅烷基酯衍生物的酯化剂。 本发明的方法产生高产率的头孢菌酸，避免了对过量的二甲基甲硅烷基化剂的需要。

    Processes for making cephems from allenylazetidinone derivatives
    25.
    发明授权
    Processes for making cephems from allenylazetidinone derivatives 失效
    从烯丙基氮杂环丁酮衍生物制备头孢烯的方法

    公开(公告)号：US5162521A

    公开(公告)日：1992-11-10

    申请号：US711250

    申请日：1991-06-06

    申请人： Vittorio Farina ,  Stephen R. Baker

    发明人： Vittorio Farina ,  Stephen R. Baker

    IPC分类号： C07D501/00 ,  C07D501/10

    CPC分类号： C07D501/00 ,  Y02P20/55

    摘要： This invention relates to a novel process for making a cephem of formula II from 2-(3-amino-2-oxo-azetidin-1-yl)-2,3-butadienoate of formula I. In another aspect, this invention is concerned with a process of further converting a compound of formula II into an antibacterial cephem of formula III. ##STR1## In formulae I, II and III, R.sup.1 is hydrogen, a conventional amino protecting group or an acyl group; R.sup.2 is an aromatic heterocyclic or aryl group; R.sup.3 is a conventional carboxy protecting group or --CO.sub.2 R.sup.3 taken together forms a physiologically hydrolyzable ester; and R.sup.4 is a group selected from the group consisting of C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, cyclic C.sub.3-6 alkyl, and aryl; and n is 0 or 2.

    摘要翻译： 本发明涉及由式I的2-（3-氨基-2-氧代 - 氮杂环丁烷-1-基）-2,3-丁二烯酸制备式II的头孢烯的新方法。另一方面，本发明涉及 其具有将式II化合物进一步转化成式III的抗菌头孢烯的方法。 在式I，II和III中，R 1是氢，常规的氨基保护基或酰基; R2是芳族杂环或芳基; R3是常规的羧基保护基或-CO 2 R 3一起形成生理上可水解的酯; 并且R 4是选自C 1-6烷基，C 2-6烯基，C 2-6炔基，环C 3-6烷基和芳基的基团。 n为0或2。

    Process for providing an oxidized penam
    27.
    发明授权
    Process for providing an oxidized penam 失效
    提供氧化的penam的方法

    公开(公告)号：US4410458A

    公开(公告)日：1983-10-18

    申请号：US328267

    申请日：1981-12-07

    申请人： Takashi Kamiya ,  Suita Saito ,  Tsutomu Teraji ,  Osamu Nakaguti ,  Teruo Oko

    发明人： Takashi Kamiya ,  Suita Saito ,  Tsutomu Teraji ,  Osamu Nakaguti ,  Teruo Oko

    IPC分类号： C07D205/08 ,  C07D205/095 ,  C07D499/00 ,  C07D499/04 ,  C07D499/21 ,  C07D499/44 ,  C07D501/10 ,  C07D501/14

    CPC分类号： C07D499/00 ,  C07D205/08 ,  C07D205/095

    摘要： This invention relates to a process for preparing an oxidized penam derivative of the formula: ##STR1## wherein R.sub.1 represents an amino or protected amino radical, andR.sub.3 represents a radical selected from the group consisting of carboxy, protected carboxy, ester, acid amide, acid anhydride, acid halide, acid azide and carboxy salt, wherein a penam derivative of the formula: ##STR2## is oxidized with an oxidizing agent selected from the group consisting of hydrogen peroxide, peracids, hydroperacids, and salts thereof, the improvement which comprises conducting said oxidation in the presence of a catalytic amount of a Group Vb or VIb of the Periodic Table metal compound.

    摘要翻译： 本发明涉及制备下式氧化的penam衍生物的方法：其中R 1表示氨基或保护的氨基，R 3表示选自羧基，被保护的羧基，酯，酰胺， 酸酐，酰卤，叠氮化物和羧基盐，其中下式的阴茎衍生物由下式的氧化剂氧化：过氧化氢，过酸，氢过酸及其盐，其改进包括 在催化量的元素周期表金属化合物的Vb或VIb族的存在下进行所述氧化。

    Process for preparing 3-methylene cephalosporins
    28.
    发明授权
    Process for preparing 3-methylene cephalosporins 失效
    制备3-亚甲基头孢菌素的方法

    公开(公告)号：US4375397A

    公开(公告)日：1983-03-01

    申请号：US666989

    申请日：1976-03-15

    申请人： Eric M. Gordon

    发明人： Eric M. Gordon

    IPC分类号： B01J19/12 ,  C07D20060101 ,  C07D501/08 ,  C07D501/10 ,  C07D501/14 ,  C07D501/22 ,  C07D501/28 ,  C07D501/30 ,  C07D513/02

    CPC分类号： C07D501/10 ,  C07D501/14

    摘要： Photolysis of azetidin-2-one derivatives having the formula ##STR1## wherein R.sub.1 is acyl, R.sub.2 is hydrogen or .alpha.-methoxy, R.sub.3 is hydrogen, alkyl, 2,2,2-trichloroethyl, trimethylsilyl, diphenylmethyl, benzyl, 4-methoxybenzyl, or 4-nitrobenzyl, and R.sub.4 is an aromatic heterocyclic group, yields 3-methylene cephalosporins.

    摘要翻译： 其中R1是酰基，R2是氢或α-甲氧基，R3是氢，烷基，2,2,2-三氯乙基，三甲基甲硅烷基，二苯基甲基，苄基，4-甲氧基苄基， 或4-硝基苄基，R4为芳香族杂环基，得到3-亚甲基头孢菌素。