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    Process for the preparation of cephradine
    1.
    发明申请
    Process for the preparation of cephradine 有权
    制备头孢拉定的方法

    公开(公告)号：US20060189802A1

    公开(公告)日：2006-08-24

    申请号：US10562345

    申请日：2004-07-01

    申请人： Dennis Heemskerk ,  Anja Gerarda Hogenboom ,  Carlos Lenhardt ,  Harold Moody ,  Theodorus Johannes Godfried Maria Dooren

    发明人： Dennis Heemskerk ,  Anja Gerarda Hogenboom ,  Carlos Lenhardt ,  Harold Moody ,  Theodorus Johannes Godfried Maria Dooren

    IPC分类号： C07D501/14

    CPC分类号： C07D501/00 ,  C12P35/04

    摘要： The present invention describes a process for preparing cephradine, said process comprising reacting 7-aminodesacetoxy cephalosporanic acid (7-ADCA) with D-dihydrophenylglycine in activated form (DHa) in the presence of an enzyme in a reaction mixture to form cephradine, resulting in a conversion of 7-ADCA into cephradine of at least 70%, wherein the concentration D-dihydrophenylglycine (DH) in the reaction mixture is below 2 wt.%, wherein the conversion of 7-ADCA into cephradine & equals; (nCEF/n7-ADCA)*100%, wherein nCEF=quantity of cephradine formed (in mole); and n7-ADCA=total quantity of 7-ADCA added to reaction mixture (in mole). The invention also describes a process for the preparation of cephradine hydrate characterised in that the process comprises: —reacting 7-amino acid desacetoxy cephalosporanic acid (7-ADCA) with DHa in the presence of an enzyme in a reaction mixture to form cephradine; —preparing an aqueous solution comprising at least part of the cephradine; and crystallising the cephradine from said aqueous solution. The invention further describes cephradine hydrate obtainable by a process according to invention. The invention also describes cephradine hydrate with an absorbance at 450 nm of below 0.050.

    摘要翻译： 本发明描述了一种制备头孢拉定的方法，所述方法包括使7-氨基二乙酰氧基头孢菌酸（7-ADCA）与活化形式的二氢苯基甘氨酸（DHa）在酶的存在下在反应混合物中反应形成头孢拉定，得到 将7-ADCA转化为至少70％的头孢拉定，其中反应混合物中D-二氢苯基甘氨酸（DH）的浓度低于2重量％，其中7-ADCA转化成头孢拉定等于; （％CEF / n 7-ADCA）* 100％，其中n CEF =形成的头孢拉定量（以摩尔计）; 和n 7-ADCA =加入到反应混合物中的7-ADCA的总量（以摩尔计）。 本发明还描述了一种制备头孢拉定水合物的方法，其特征在于该方法包括：在反应混合物中，在酶的存在下，用7-氨基酸脱乙酰氧基头孢菌酸（7-ADCA）与DHa反应形成头孢拉定; - 制备包含至少一部分头孢拉定的水溶液; 并从所述水溶液中结晶头孢拉定。 本发明还描述了通过根据本发明的方法获得的头孢拉定水合物。 本发明还描述了在450nm处的吸光度低于0.050的头孢拉定水合物。

    D-amino acid aminotransferase for simultaneously producing glutaryl-7-aminocephalosporanic acid and D-amino acid
    2.
    发明授权
    D-amino acid aminotransferase for simultaneously producing glutaryl-7-aminocephalosporanic acid and D-amino acid 失效
    同时生产戊二酰-7-氨基头孢烷酸和D-氨基酸的D-氨基酸氨基转移酶

    公开(公告)号：US06337190B1

    公开(公告)日：2002-01-08

    申请号：US09466257

    申请日：1999-12-17

    申请人： Tzann-Shun Hwang ,  Szu-Pei Wu ,  Hsin-Hua Chou ,  Hwa-Yi Chen ,  Lung-Shen Lin ,  Hsin Tsai ,  Edward Chang

    发明人： Tzann-Shun Hwang ,  Szu-Pei Wu ,  Hsin-Hua Chou ,  Hwa-Yi Chen ,  Lung-Shen Lin ,  Hsin Tsai ,  Edward Chang

    IPC分类号： C12N900

    CPC分类号： C12N9/1096 ,  C12P35/04

    摘要： The present invention relates to mutant D-amino acid aminotransferase, including nucleic acids encoding mutant D-amino acid aminotransferase. The mutant D-amino acid aminotransferase of the present invention is obtained by the substitution of the glutamate residue at position 13 of wild type D-amino acid aminotransferase from Bacillus sphaericus with hydrophobic amino acids. The mutant D-amino acid aminotransferase can be used in the production of D-amino acid and the conversion of glutaryl-7-aminocephalosporanic acid from cephalosporin C. The present invention also includes replica-paper staining method for screening the cells expressing high DAT activity.

    摘要翻译： 本发明涉及突变型D-氨基酸氨基转移酶，包括编码突变型D-氨基酸氨基转移酶的核酸。 通过用疏水性氨基酸取代来自球形芽孢杆菌的野生型D-氨基酸氨基转移酶的13位的谷氨酸残基获得本发明的突变型D-氨基酸氨基转移酶。 突变型D-氨基酸氨基转移酶可用于D-氨基酸的生产和戊二酰-7-氨基头孢菌酸从头孢菌素C的转化。本发明还包括用于筛选表达高DAT活性的细胞的复制纸染色方法 。

    Process for the preparation of a&bgr;-lactam antibiotic
    3.
    发明授权
    Process for the preparation of a&bgr;-lactam antibiotic 失效
    制备abeta-lactam抗生素的方法

    公开(公告)号：US06287799B1

    公开(公告)日：2001-09-11

    申请号：US09529569

    申请日：2000-04-18

    申请人： Theodorus Johannes Godfried Marie Van Dooren ,  Johanna Christina Maria Smeets ,  Harold Monro Moody

    发明人： Theodorus Johannes Godfried Marie Van Dooren ,  Johanna Christina Maria Smeets ,  Harold Monro Moody

    IPC分类号： C12P3504

    CPC分类号： C12P35/04 ,  C12P37/04

    摘要： Process for the preparation of a &bgr;-lactam antibiotic in which a &bgr;-lactam nucleus is subjected to an enzymatic acylation reaction with the aid of an acylation agent at a molar ratio of acylation agent/&bgr;-lactam nucleus of less than 2.5, with the acylation agent and/or the &bgr;-lactam nucleus being supersaturated in the reaction mixture during at least part of the acylation reaction. In the process, a concentrated slurry or solution, for instance, of the &bgr;-lactam nucleus and/or the acylation agent with a different pH or a higher temperature than the pH or temperature at which the acylation reaction is carried out is added to the reaction mixture during the acylation reaction. Both the &bgr;-lactam nucleus and the acylation agent may be supersaturated in the reaction mixture.

    摘要翻译： 制备β-内酰胺抗生素的方法，其中β-内酰胺核在借助于酰化剂的酰化剂/β-内酰胺核的摩尔比小于2.5的条件下进行酶酰化反应，其中 酰化剂和/或β-内酰胺核在至少部分酰化反应中在反应混合物中过饱和。 在此过程中，将浓缩的浆液或溶液，例如β-内酰胺核和/或具有与进行酰化反应的pH或温度不同的pH或更高温度的酰化剂加入到 酰化反应中的反应混合物。 β-内酰胺核和酰化剂都可以在反应混合物中过饱和。

    Process for preparing cephalosporins with penicillin acylase without pH control
    4.
    发明授权
    Process for preparing cephalosporins with penicillin acylase without pH control 失效
    用于无pH控制的青霉素酰基转移酶制备头孢菌素的方法

    公开(公告)号：US5801011A

    公开(公告)日：1998-09-01

    申请号：US588148

    申请日：1996-01-18

    申请人： John P. Gardner

    发明人： John P. Gardner

    IPC分类号： C07D501/06 ,  C07D501/24 ,  C12P35/04 ,  C12P35/06 ,  C12P35/00

    CPC分类号： C12P35/04

    摘要： The invention relates to an improved process for preparing cephalosporins by reaction compounds such as 7-amino-cephalosporanic acid, 7-amino-3-deacetoxy-cephalosporanic acid or their derivatives with derivatives of .alpha.-amino acids in the presence of a properly immobilized penicillin acylase enzyme under the following conditions, independently, or in combination: (1) at a temperature ranging from 0.degree. C. to +20.degree. C.; or (2) at ambient pH; with a high molar ratio of .alpha.-amino acid to a cephalosporanic nucleus.

    摘要翻译： 本发明涉及一种通过反应化合物如7-氨基 - 头孢烷酸，7-氨基-3-脱乙酰氧基 - 头孢菌酸或其衍生物与α-氨基酸衍生物在适当固定的青霉素存在下制备头孢菌素的改进方法 酰化酶在以下条件下独立地或组合使用：（1）在0℃至+ 20℃的温度范围内。 或（2）在环境pH下; 具有高摩尔比的α-氨基酸与头孢菌素核。

    Production of antibacterial agents
    6.
    发明授权
    Production of antibacterial agents 失效
    生产抗菌剂

    公开(公告)号：US3899394A

    公开(公告)日：1975-08-12

    申请号：US43950874

    申请日：1974-02-21

    申请人： BRISTOL MYERS CO

    发明人： WILLNER DAVID ,  CRAST JR LEONARD BRUCE

    IPC分类号： C12P35/04 ,  C12D1/00

    CPC分类号： C07D501/36 ,  C12P35/04 ,  Y10S435/823 ,  Y10S435/874 ,  Y10S435/91

    摘要： 7-(D Alpha -Amino- Alpha -(p-hydroxyphenyl)acetamido)-3-(1,2,3triazol-5-ylthiomethyl)-3-cephem-4 -carboxylic acid and its nontoxic, pharmaceutically acceptable salts exhibit highly desirable solubility in water, are efficiently absorbed on oral administration to provide relatively high and prolonged blood levels and are potent antibacterial agents useful in the treatment of infectious diseases in animals, including man, caused by many Gram-positive and Gram-negative bacteria. 7-(D- Alpha -Amino- Alpha -(p-hydroxyphenyl)acetamido)-3-(1,2,3triazol-5-ylthiomethyl)-3-cephem-4 -carboxylic acid is prepared, for example, by contacting methyl D-(-)- Alpha -amino- Alpha -(4hydroxyphenyl)acetate or an acid addition salt thereof with 7amino-3-(1,2,3-triazol-5-ylthiomethyl)-3-cephem-4-carboxylic acid or a salt thereof in aqueous solution in the presence of enzyme derived from a microorganism selected from the group consisting of Xanthomonas citri (IFO 3835), Acetobacter turbidans (ATCC 9325) and Pseudomonas melanogenum (IFO 12020).

    摘要翻译： 7- [Dα-氨基-α-（对羟基苯基）乙酰氨基] -3-（1,2,3-三唑-5-基硫甲基）-3-头孢烯-4-羧酸及其无毒的药学上可接受的盐展示 在水中非常理想的溶解度在口服给药时被有效地吸收以提供相对较高和延长的血液水平，并且是用于治疗由许多革兰氏阳性和革兰氏阴性菌引起的包括人在内的动物感染性疾病的有效的抗菌剂。

    METHOD FOR PREPARING A BETA-LACTAM ANTIBIOTIC
    8.
    发明申请
    METHOD FOR PREPARING A BETA-LACTAM ANTIBIOTIC 无效
    制备BETA-LACTAM抗生素的方法

    公开(公告)号：US20020006642A1

    公开(公告)日：2002-01-17

    申请号：US09202799

    申请日：1999-05-03

    发明人： THOMAS VAN DER DOES ,  JAGDISH CHANDER KAPUR ,  ERIK DE VROOM

    IPC分类号： C12P037/04 ,  C12P021/04

    CPC分类号： C12P37/04 ,  C12P35/02 ,  C12P35/04 ,  C12P37/06

    摘要： The invention relates to a method for preparing a null-lactam antibiotic, wherein an N-substituted null-lactam, having general formula (I), wherein R0 is hydrogen or C1-3 alkoxy; Y is CH2, oxygen, sulfur, or an oxidized form of sulfur; Z is (a), (b), (c) or (d), wherein R1 is hydrogen, hydroxy, halogen, C1-3 alkoxy, optionally substituted, optionally containing one or more heteroatoms, saturated or unsaturated, branched or straight C1-5 alkyl, preferably methyl, optionally substituted, optionally containing one or more heteroatoms C5-8 cycloalkyl, optionally substituted aryl or heteroaryl, or optionally substituted benzyl; and X is (CH2)m-A-(CH2)n, wherein m and n are the same or different and are chosen from the group of integers 0, 1, 2, 3 or 4 and A is CHnullCH, CnullC, CHB, CnullO, optionally substituted nitrogen, oxygen, sulfur or an optionally oxidized form of sulfur, and B is hydrogen, halogen, hydroxy, C1-3 alkoxy, or optionally substituted methyl, or a salt thereof, is contacted with at least one dicarboxylate acylase, or a functional equivalent thereof, and reacted with a precursor for a side chain of the null-lactam antibiotic in the presence of at least one penicillin acylase, or a functional equivalent thereof.

    摘要翻译： 本发明涉及一种制备β-内酰胺抗生素的方法，其中具有通式（I）的N-取代的β-内酰胺，其中R 0是氢或C 1-3烷氧基; Y是CH 2，氧，硫或硫的氧化形式; Z是（a），（b），（c）或（d），其中R 1是氢，羟基，卤素，C 1-3烷氧基，任选地被取代，任选地含有一个或多个杂原子，饱和或不饱和的，支链或直链C1 -5烷基，优选甲基，任选地被取代，任选地含有一个或多个杂原子C5-8环烷基，任选取代的芳基或杂芳基，或任选取代的苄基; 并且X是（CH 2）mA-（CH 2）n，其中m和n相同或不同，并且选自整数0,1,2,3或4，A是CH = CH，C = C， CHB，C = O，任选取代的氮，氧，硫或任选氧化形式的硫，B是氢，卤素，羟基，C 1-3烷氧基或任选取代的甲基或其盐与至少 一种二羧酸酰基转移酶或其功能等同物，并且在至少一种青霉素酰基转移酶或其功能等同物的存在下与β-内酰胺抗生素的侧链的前体反应。

    Synthesis of beta-lactam antibiotics with immobilized penicillin amidase
    9.
    发明授权
    Synthesis of beta-lactam antibiotics with immobilized penicillin amidase 失效
    用固定青霉素酰胺酶合成β-内酰胺抗生素

    公开(公告)号：US06218138B1

    公开(公告)日：2001-04-17

    申请号：US09318732

    申请日：1999-05-26

    申请人： Ferhat Ilhan ,  Dieter Kraemer

    发明人： Ferhat Ilhan ,  Dieter Kraemer

    IPC分类号： C12P3704

    CPC分类号： C12P37/04 ,  C12P35/04

    摘要： Beta-lactam antibiotics are synthesized by reacting an amino-beta-lactam component with a corresponding amino-group-containing acylating side-chain component in the presence of penicillin amidase from E. coli covalently immobilized on support particles. The resulting beta-lactam antibiotic product is solubilized by adding an acid such as sulfuric acid to lower the pH to 1.0 at a temperature in the range of 0° C. to +5° C. The immobilized penicillin amidase is substantially inactivated by the acid. After separating the beta-lactam antibiotic product, the immobilized penicillin amidase is substantially reactivated for reuse in antibiotic synthesis by treatment with a buffer having about a neutral pH. Antibiotics that can be produced include ampicillin, amoxicillin, cephalexin, cefaclor and cefadroxil. Support particles that can be used include particles having a macroporous structure and a particle diameter of 10-1000 &mgr;m, particles having oxirane groups, particles made of a synthetic polymer and inorganic particles such as porous glass particles.

    摘要翻译： β-内酰胺抗生素通过氨基-β-内酰胺组分与相应的含氨基酰化侧链组分在共价固定在载体颗粒上的大肠杆菌的青霉素酰胺酶存在下反应而合成。 所得β-内酰胺抗生素产品通过加入酸如硫酸溶解，在0℃至+ 5℃的温度范围内将pH降至1.0。固定的青霉素酰胺酶基本上被酸灭活 。 在分离β-内酰胺抗生素产物之后，通过用具有约中性pH的缓冲液处理，固定化的青霉素酰胺酶基本上被再活化用于抗生素合成中的再利用。 可生产的抗生素包括氨苄青霉素，阿莫西林，头孢氨苄，头孢克洛和头孢羟氨苄。 可以使用的载体颗粒包括具有大孔结构，粒径为10-1000μm的颗粒，具有环氧乙烷基团的颗粒，由合成聚合物制成的颗粒和无机颗粒如多孔玻璃颗粒。