Penicillin oxidation process
    81.
    发明授权
    Penicillin oxidation process 失效
    泼尼松素氧化过程

    公开(公告)号:US3904605A

    公开(公告)日:1975-09-09

    申请号:US28845972

    申请日:1972-09-12

    申请人: LILLY CO ELI

    发明人: BAKER PATRICK J

    CPC分类号: C07D499/00

    摘要: Penicillin sulfoxide acid is obtained in higher, more economical yield and of surprisingly good purity from penicillin in fermentation filtered broth by concentrating the broth, diluting the concentrated broth with miscible organic liquid, optionally separating insolubles, treating the liquid mixture with a peracid oxidizing agent to form sulfoxide, adjusting the ph of the mixture to 1.5 to 2.5, and crystallizing the penicillin sulfoxide acid, with the aid of additional water, if necessary, and separating the solid penicillin sulfoxide.

    Thiadiazolyl amino penicillins
    83.
    发明授权
    Thiadiazolyl amino penicillins 失效
    三氨基苯胺氨基酸

    公开(公告)号:US3816411A

    公开(公告)日:1974-06-11

    申请号:US17139771

    申请日:1971-08-12

    CPC分类号: C07D285/10 C07D499/00

    摘要: A PROCESS FOR THE PREPARATION OF A PENICILLIN COMPOUND OF A SALT THEREOF THE FORMULA I

    2-(HOOC-),3,3-DI(CH3-),6-((4-A-1,2,5-THIADIAZOL-3-YL)-Y-

    C(-B)(-X)-CO-NH-)PENAM

    WHEREIN A IS HYDROGEN, ALKYL HAVING 1 TO 4 CARBON ATOMS, ARALKYL SELECTED FROM THE GROUP WHICH CONSISTS OF BENZYL AND PHENYLETHYL UNSUBSTITUTED OR SUBSTITUTED WITH CHLORO, METHOXY OR ETHOXY, OR ARYL SELECTED FROM THE GROUP WICH CONSISTS OF PHENYL AND NAPHTHYL UNSUBSTITUED OR SUBSTITUTED WITH CHLORINE, METHOXY OR ETHOXY; B IS HYDROGEN OR ALKYL HAVING 1 TO 4 CARBON ATOMS, Y IS OXYGEN OR SULFUR, X IS HYDROGEN OR ALKYL HAVING 1 TO 4 CARBON ATOMS, WHICH COMPRISES REACTING 6-AMINOPENICILLANIC ACID OR A TRIALKYLXYLYL ESTER THEREOF WITH A CARBOXYLIC ACID OF THE FORMULA II

    3-(HOOC-C(-B)(-X)-Y-),4-A-1,2,5-THIADIAZOLE

    OR A REACTIVE DERIVATIVE THEREOF SELECTED THE GROUP WHICH CONSISTS OF THE AZIDES, ACID CHLORIDES, ACID BROMIDES AND HYDRIDES OF SAID CARBOXYLIC ACID.

    6-(3-aryl-1,2,4-oxadiazole-5-one-4-acet-amido)penicillanic acids
    84.
    发明授权
    6-(3-aryl-1,2,4-oxadiazole-5-one-4-acet-amido)penicillanic acids 失效
    6-(3-氰基-1,2,4-氧杂噻唑-5-酮-4-乙酰氨基)苯胺

    公开(公告)号:US3767646A

    公开(公告)日:1973-10-23

    申请号:US3767646D

    申请日:1971-11-29

    申请人: BRISTOL MYERS CO

    发明人: TRUMAN HOLDREGE C

    摘要: 6-(N - (SUBSTITUTED - IMIDOYL) AMINOACETAMIDO)PENICILLANIC ACIDS AND THEIR SALTS ARE VALUABLE AS ANTIBACTERIAL AGENTS, NUTRITIONAL SUPPLEMENTS IN ANIMAL FEEDS, THERAPEUTIC AGENTS IN POULTRY AND ANIMALS, INCLUDING MAN, AND ARE ESPECIALLY USEFUL IN THE TREATMENT OF INFECTIOUS DISEASES CAUSED BY GRAM-POSITIVE AND CERTAIN GRAM-NEGATIVE BACTERIA, MOST PARTICULARLY THOSE CAUSED BY THE PROTEUS GENUS. 6-(N-PHENYLACETIMIDOYL) - AMINOACETAMIDO)PENICILLANIC ACID, A PREFERRED EMBODIMENT OF THE INVENTION, IS PREPARED BY RANEY NICKEL HYDROGENATION (50 P.S.I., R.T.) OF AQUEOUS SOLUTION OF SODIUM 6-(3-BENZYL-1,2,4-OXADIAZOLE-5ONE-4-ACETAMIDO)PENICILLANATE WHICH IS PREPARED IN TURN BY REACTION OF 6-AMINOPENICILLANIC ACID WITH 3-BENZYL-1,2, 4-OXADIAZOLE-5-ONE-4-ACETYL CHLORIDE.

    Process for acetylation
    85.
    发明授权
    Process for acetylation 失效
    乙酰化方法

    公开(公告)号:US3715347A

    公开(公告)日:1973-02-06

    申请号:US3715347D

    申请日:1970-11-06

    申请人: LILLY CO ELI

    发明人: SPRY D WRIGHT I

    CPC分类号: C07D499/00

    摘要: 6-Aminopenicillanic acid, 3-acetoxymethyl-7-amino- Delta 3cephem-4-carboxylic acid and 3-methyl-7-amino- Delta 3-cephem-4car-boxylic acid and esters thereof are reacted with ketene in an aqueous or inert non-aqueous solvent at a temperature between about 5* and about 35* C. to provide the corresponding acetamido derivatives in superior yields. 6-Acetamidopenicillanic acid, 3acetoxymethyl-7-acetamido- Delta 3-cephem-4-carboxylic acid, 3methyl-7-acetamido- Delta 3-cephem-4-carboxylic acid and the esters thereof are useful intermediates for the preparation of cephalosporin antibiotics.

    摘要翻译: 将6-氨基青霉烷酸,3-乙酰氧基甲基-7-氨基-D-TA-头孢烯-4-羧酸和3-甲基-7-氨基-Detta 3-头孢烯-4-羧酸和其酯与乙烯酮反应 水溶液或惰性非水溶剂,温度在约5℃至约35℃之间,以优异的产率提供相应的乙酰氨基衍生物。 6-乙酰氨基青霉烷酸,3-乙酰氧基甲基-7-乙酰氨基-Detta 3-头孢烯-4-羧酸,3-甲基-7-乙酰氨基-D-3头孢烯-4-羧酸及其酯是制备中的有用的中间体 的头孢菌素抗生素。