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    Simple enzymatic process for preparing cefazolin
    1.
    发明公开
    Simple enzymatic process for preparing cefazolin 有权
    Einfach酶促Verfahren zur Herstellung von Cefazolin

    公开(公告)号：EP1416054A1

    公开(公告)日：2004-05-06

    申请号：EP02380224.2

    申请日：2002-10-31

    申请人： Bioferma Murcia, S.A.

    发明人： Sanchez Ferrer, Alvaro ,  Garcia Carmona, Francisco

    IPC分类号： C12P35/04 ,  C12N9/84 ,  C07D501/36

    CPC分类号： C12Y305/01011 ,  C12P35/04

    摘要： A process for preparing the 7-(1-H-tetrazol-1-yl) acetamide-3-(2-methyl-1,3,4-thiadiazol-5-yl)thiomethyl-3-cephem-4-carboxylic acid or cefazolin, comprising catalysing the acylation of the amino β-lactam, the 7-amino-3-[5methyl-1,3,4-thiadiazol-2-yl)thiomethyl]-3-cephem-4-carboxylic acid, of the formula with an activated acylating agent derived from acetic acid in the presence of a biocatalyst comprising penicillin amidase, and a product of the formula I obtainable by the foregoing process according to claims.

    摘要翻译： 头孢唑啉（A）的制备涉及在生物催化剂存在下，将含有四氢乙酸的7-氨基-3 - [（甲基-1,3,4-噻二唑-2-基）硫甲基] -3-头孢烯-4-羧酸酰化 含量为6-8和-20-40℃的青霉素酰胺酶; 并在0-20℃下通过加入酸将pH降低到3.5以下使（A）沉淀。 头孢唑啉（A）的制备涉及用含有四氢的乙酸将7-氨基-3 - [（甲基-1,3,4-噻二唑-2-基）硫代甲基] -3-头孢烯-4-羧酸（I）或其盐 在含有生物催化剂的青霉素酰胺酶（EC 3.5.1.11）（100-50000单位/升）存在下，pH为6-8和-20-40（优选0-10）℃下，式（II）的酸 ; 并通过在0-20℃下加入酸以降低pH低于3.5而沉淀（A）。 R：酸的酯或酰胺。 活性：抗生素。 没有给出生物数据。 行动机制：无给予。

    SIMPLE ENZYMATIC PROCESS FOR PREPARING CEFAZOLIN
    2.
    发明公开
    SIMPLE ENZYMATIC PROCESS FOR PREPARING CEFAZOLIN 审中-公开
    SIMPLE酶解过程用于生产CEFALOZOLIN

    公开(公告)号：EP1556500A1

    公开(公告)日：2005-07-27

    申请号：EP03773688.1

    申请日：2003-10-30

    申请人： Bioferma Murcia, S.A.

    发明人： GARCIA CARMONA, Francisco ,  SANCHEZ FERRER, Alvaro

    IPC分类号： C12P35/04 ,  C12N9/84 ,  C07D501/36

    CPC分类号： C12Y305/01011 ,  C12P35/04

    摘要： A process for preparing the 7-(1-H-tetrazol-1-yl) acetamide-3-(2-methyl-1,3,4-thiadiazol-5-yl)thiomethyl-3-cephem-4-carboxylic acid or cefazolin, comprising catalysing the acylation of the amino β-lactam, the 7-amino-3-[5methyl-1,3,4-thiadiazol-2-yl)thiomethyl]-3-cephem-4-carboxylic acid, of the formula with an activated acylating agent derived from acetic acid in the presence of a biocatalyst comprising penicillin amidase, and a product of the formula I obtainable by the foregoing process according to claims.

    An enzymatic process for preparing beta-lactams
    3.
    发明公开
    An enzymatic process for preparing beta-lactams 审中-公开
    Enzymatischer Prozess zur Herstellung von beta-Lactamverbindungen

    公开(公告)号：EP1394262A1

    公开(公告)日：2004-03-03

    申请号：EP02078608.3

    申请日：2002-08-30

    申请人： Bioferma Murcia, S.A.

    发明人： Giesecke, Ulrich Eberhard

    IPC分类号： C12P35/04 ,  C12P35/00 ,  C12P35/02

    CPC分类号： C12P35/00 ,  C12P35/02 ,  C12P35/04

    摘要： An enzymatic process for preparing β-lactams, by coupling the 7-amino group of a cephalosporin nucleus with the carboxylic function of an acetic acid derivative consisting of a residue with π-electrons, a short spacer and a carboxylic function or derivative. The process comprises using a penicillin amidase or α-amino acid esterase as free enzyme or in any suitable immobilised form; applying no or maximum 10 % organic solvent, applying at least 100 mmol/l cephalosporin nucleus as long as it is soluble, otherwise 50 - 100 % of its maximum solubility is charged, applying the free organic acid in a 3 - 5 fold molar ratio or activated as ester or amide in a 1 - 3 fold molar ratio, and adjusting the pH to 5.0 - 8.0 and the temperature to 0 - 40°C.

    摘要翻译： 通过将头孢菌素核的7-氨基与由残留物组成的乙酸衍生物的π-电子，短间隔子和羧基官能团或衍生物的羧酸官能团结合来制备β-内酰胺的酶促方法。 该方法包括使用青霉素酰胺酶或α-氨基酸酯酶作为游离酶或以任何合适的固定形式; 施用无或最多10％的有机溶剂，只要溶解至少100mmol / l头孢菌素核，否则加入其最大溶解度的50-100％，加入3〜5倍摩尔比的游离有机酸 或以1-3倍摩尔比的酯或酰胺活化，并将pH调节至5.0-8.0和温度至0-40℃。

    ENZYMATIC PROCESS FOR PREPARING CEPHALOSPORANIC ACID DERIVATIVES USING ALPHA-KETOACID DERIVATIVES
    5.
    发明公开
    ENZYMATIC PROCESS FOR PREPARING CEPHALOSPORANIC ACID DERIVATIVES USING ALPHA-KETOACID DERIVATIVES 审中-公开
    用α-酮酸衍生物制备头孢烯酸衍生物的酶法

    公开(公告)号：EP1379531A2

    公开(公告)日：2004-01-14

    申请号：EP02735276.4

    申请日：2002-04-18

    申请人： Bioferma Murcia, S.A.

    发明人： SANCHEZ-FERRER, Alvaro ,  LOPEZ-MAS, Jose Aniceto ,  GARCIA-CARMONA, Francisco

    IPC分类号： C07D501/04 ,  C07D501/36 ,  C12P35/06

    CPC分类号： C07D501/00

    摘要： A process for preparing cephalosporanic acid derivatives comprises the steps of enzymatically converting a 3-thiolated cephalosporin C compound of formula (III) into a 3-thiolated-α-ketoadipyl-7-aminocephalosporanic acid derivative of formula (IV), wherein R is a heterocyclic group comprising at least a nitrogen atom. Compounds of formula (IV) are used in the preparation of cephalosporin C antibiotics and derivatives thereof.

    摘要翻译： 制备头孢菌酸衍生物的方法包括以下步骤：将式（III）的3-硫醇化头孢菌素C化合物酶促转化成式（IV）的3-硫醇化-α-酮基己二酰-7-氨基头孢菌酸衍生物，其中R是 包含至少一个氮原子的杂环基团。 式（IV）化合物用于制备头孢菌素C抗生素及其衍生物。