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公开(公告)号：WO2012175587A2
公开(公告)日：2012-12-27
申请号：PCT/EP2012/061912
申请日：2012-06-21
Applicant: DSM Sinochem Pharmaceuticals Netherlands B.V. , MOODY, Harold, Monro , CUSAN, Claudia , IJPEIJ, Edwin, Gerard
Inventor： MOODY, Harold, Monro , CUSAN, Claudia , IJPEIJ, Edwin, Gerard
IPC: C12P35/04 , C07D501/24 , A61K31/545 , A61P31/04
CPC classification number: C07D501/24 , A61K31/545 , C12P35/04
Abstract: The present invention relates to a crystalline form of an intermediate for cefoperazone of formula (1 ) and to a process for the preparation thereof by enzymatic condensation of a 3'-thiosubstituted β-lactam nucleus with a phenylglycine derivative.
Abstract translation: 本发明涉及式（1）的头孢哌酮的中间体的结晶形式及其通过3'-取代的β-内酰胺核与苯基甘氨酸衍生物的酶缩缩来制备的方法。
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公开(公告)号：WO2011073166A2
公开(公告)日：2011-06-23
申请号：PCT/EP2010/069575
申请日：2010-12-14
Applicant: DSM IP ASSETS B.V. , MOODY, Harold, Monro , DOOREN, VAN, Theodorus, Johannes, Godfried, Maria
IPC: C12P35/04
CPC classification number: C12P35/04 , C12Y305/01011
Abstract: The invention relates to a process for preparing cephradine, said process comprising converting D-dihydrophenylglycine (DHPG) into an activated form (DHPGa); and reacting 7-aminodesacetoxy-cephalosporanic acid (7-ADCA) with D- dihydrophenylglycine in activated form (DHPGa) in the presence of an enzyme in an aqueous reaction mixture to form cephradine characterized in that at least step (a) and step (b) of the process are carried out under anaerobic conditions.
Abstract translation: 本发明涉及一种制备头孢拉定的方法，所述方法包括将D-二氢苯基甘氨酸（DHPG）转化为活化形式（DHPGa）; 并在酶水解反应混合物中使7-氨基二乙酰氧基 - 头孢菌酸（7-ADCA）与活性形式的D-二氢苯基甘氨酸（DHPGa）反应，形成头孢拉定，其特征在于至少步骤（a）和步骤（b ）的过程在厌氧条件下进行。
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公开(公告)号：WO2004020651A1
公开(公告)日：2004-03-11
申请号：PCT/EP2003/009660
申请日：2003-08-29
Applicant: BIOFERMA MURCIA, S.A. , GIESECKE, Ulrich, Eberhard
Inventor： GIESECKE, Ulrich, Eberhard
IPC: C12P35/04
Abstract: An enzymatic process under kinetical control 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 activated as hydroxyethylester. The process comprises using a penicillin amidase or α-amino acid esterase as free enzyme or in any suitable immobilised form; applying at least 100 mmol/l cephalosporin nucleus, applying the acetic acid derivative activated as hydroxyethylester in a 1 - 3 fold molar ratio, and adjusting the pH to 6.0 - 8.0 and the temperature to 0 - 30°C.
Abstract translation: 在动力学控制下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的羧基官能团偶联而制备β-内酰胺的酶法 hydroxyethylester。 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; 施用至少100mmol / l头孢菌素核，以1-3倍摩尔比施用活化为羟乙基酯的乙酸衍生物，并将pH调节至6.0-8.0，温度为0-30℃。
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公开(公告)号：WO99020786A1
公开(公告)日：1999-04-29
申请号：PCT/NL1998/000570
申请日：1998-10-01
Abstract: Process for the preparation of a beta -lactam antibiotic in which a beta -lactam nucleus is subjected to an enzymatic acylation reaction with the aid of an acylation agent at a molar ratio of acylation agent/ beta -lactam nucleus of less than 2.5, with the acylation agent and/or the beta -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 beta -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 beta -lactam nucleus and the acylation agent may be supersaturated in the reaction mixture.
Abstract translation: 用于制备β-内酰胺抗生素的方法，其中β-内酰胺核在借助酰化剂以酰基化试剂/β-内酰胺核的摩尔比小于2.5进行酶促酰化反应，其中 酰化剂和/或β-内酰胺核在反应混合物中至少部分酰化反应过饱和。 在此过程中，将浓缩的浆液或溶液，例如与实施酰化反应的pH或温度不同的pH或更高温度的β-内酰胺核和/或酰化剂加入到 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。
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5.发明申请METHOD FOR THE SYNTHESIS OF SEMI-SYNTHETIC ANTIBIOTICS IN THERMODYNAMICALLY CONTROLLED WATER-COSOLVENT ORGANIC MISCIBLE APOLAR SYSTEMS BY USING PENICILLIN G ACYLASE 审中-公开通过使用PENICILLIN G ACYLASE在热力学控制的水有机有机无机系统中合成半合成抗生素的方法
公开(公告)号：WO1991009136A1
公开(公告)日：1991-06-27
申请号：PCT/ES1990000046
申请日：1990-12-12
Applicant: CONSEJO SUPERIOR INVESTIGACIONES CIENTIFICAS , GUISAN SEIJAS, José, M.; , FERNANDEZ-LAFUENTE, Roberto; , ALVARO CAMPOS, Gregorio; , BLANCO MARTIN, Rosa, Mª; , MOLINA ROSELL, Cristina;
IPC: C12P35/04
Abstract: Synthesis of semi-synthetic monobactamic or beta -lactamic antibiotics by using derivatives stabilized by various methods of penicillin G acylase from various microbial sources according to a thermodynamically controlled strategy in monophase water/cosolvent organic apolar systems, wherein the concentration of the cosolvent varies between 30 % and 90 %, the temperature between -10 DEG C and 50 DEG C, the pH between 4.5 and 8.5, with concentrations of the antibiotic nucleus between 0.5 and 875 mM and acyl donor between 0.2 mM and 1 M, with a relationship antibiotic ring/activated or free acyl donor, using a buffer between 0 and 1 M. Application to the pharmaceutical industry.
Abstract translation: 根据单相水/助溶剂有机非极性体系中的热力学控制策略，通过使用通过各种微生物来源的各种青霉素G酰基转移酶稳定的衍生物合成半合成单体或β-乳酸抗生素，其中助溶剂的浓度在30 ％和90％，温度在-10℃和50℃之间，pH在4.5和8.5之间，抗生素核的浓度在0.5和875mM之间，酰基供体在0.2mM和1M之间，具有关系抗生素环 /活化或游离酰基供体，使用0和1 M之间的缓冲液。应用于制药工业。
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Patent Agency Ranking6.发明申请CRYSTALLINE CEFOPERAZONE INTERMEDIATE, PROCESS FOR ITS PREPARATION AND PHARMACEUTICAL USE THEREOF 审中-公开晶体蛋白酶中间体，其制备方法及其药物应用
公开(公告)号：WO2012175587A3
公开(公告)日：2013-03-28
申请号：PCT/EP2012061912
申请日：2012-06-21
Applicant: DSM SINOCHEM PHARM NL BV , MOODY HAROLD MONRO , CUSAN CLAUDIA , IJPEIJ EDWIN GERARD
Inventor： MOODY HAROLD MONRO , CUSAN CLAUDIA , IJPEIJ EDWIN GERARD
IPC: C12P35/04 , A61K31/545 , A61P31/04 , C07D501/24
CPC classification number: C07D501/24 , A61K31/545 , C12P35/04
Abstract: The present invention relates to a crystalline form of an intermediate for cefoperazone of formula (1 ) and to a process for the preparation thereof by enzymatic condensation of a 3'-thiosubstituted beta-lactam nucleus with a phenylglycine derivative.
Abstract translation: 本发明涉及式（1）的头孢哌酮的中间体的结晶形式，以及通过3'-取代的β-内酰胺核与苯基甘氨酸衍生物的酶缩缩来制备其的方法。
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公开(公告)号：WO2011073166A3
公开(公告)日：2011-09-15
申请号：PCT/EP2010069575
申请日：2010-12-14
IPC: C12P35/04
CPC classification number: C12P35/04 , C12Y305/01011
Abstract: The invention relates to a process for preparing cephradine, said process comprising converting D-dihydrophenylglycine (DHPG) into an activated form (DHPGa); and reacting 7-aminodesacetoxy-cephalosporanic acid (7-ADCA) with D- dihydrophenylglycine in activated form (DHPGa) in the presence of an enzyme in an aqueous reaction mixture to form cephradine characterized in that at least step (a) and step (b) of the process are carried out under anaerobic conditions.
Abstract translation: 本发明涉及一种制备头孢拉定的方法，所述方法包括将D-二氢苯基甘氨酸（DHPG）转化成活化形式（DHPGa）; 和使7-氨基去乙酰氧基头孢烷酸（7-ADCA）与活化形式的D-二氢苯基甘氨酸（DHPGa）在酶的存在下在含水反应混合物中反应以形成头孢拉定，其特征在于至少步骤（a）和步骤（b ）的过程在厌氧条件下进行。
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公开(公告)号：WO2004039997A1
公开(公告)日：2004-05-13
申请号：PCT/EP2003/012165
申请日：2003-10-30
Applicant: BIOFERMA MURCIA, S.A. , GARCIA CARMONA, Francisco , SANCHEZ FERRER, Alvaro
Inventor： GARCIA CARMONA, Francisco , SANCHEZ FERRER, Alvaro
IPC: C12P35/04
CPC classification number: C12Y305/01011 , C12P35/04
Abstract: 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.
Abstract translation: 制备7-（1-H-四唑-1-基）乙酰胺-3-（2-甲基-1,3,4-噻二唑-5-基）硫甲基-3-头孢烯-4-羧酸的方法或 头孢唑啉，其包括催化氨基β-内酰胺的酰化，7-氨基-3- [5-甲基-1,3,4-噻二唑-2-基]硫甲基] -3-头孢烯-4-羧酸的式 在含有青霉素酰胺酶的生物催化剂存在下由乙酸衍生的活化酰化剂，以及通过根据权利要求的前述方法可得到的式I的产物。
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公开(公告)号：WO2004020649A1
公开(公告)日：2004-03-11
申请号：PCT/EP2003/009658
申请日：2003-08-29
Applicant: BIOFERMA MURCIA, S.A. , GIESECKE, Ulrich, Eberhard
Inventor： GIESECKE, Ulrich, Eberhard
IPC: C12P35/04
Abstract: An enzymatic process under thermodynamical control for preparing b-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 p-electrons, a short spacer and a carboxylic function. The process comprises using a penicillin amidase as free enzyme or in any suitable immobilised form; applying no or maximum 10 % organic solvent, applying at least 100 mmol/l cephalosporin nucleus, applying the free acetic acid derivative in a 3 - 5 fold molar ratio, reducing the pH by acid according the reaction progress from initially pH 7.5 - 6.25 to pH 6.25 - 5.0 and adjusting 10 - 40°C.
Abstract translation: 通过将头孢菌素核的7-氨基与由p电子组成的残基的乙酸衍生物，短间隔子和羧基官能团的羧基官能团偶联，制备β-内酰胺的热力学控制下的酶学方法。 该方法包括使用青霉素酰胺酶作为游离酶或以任何合适的固定形式; 施用无或最高10％的有机溶剂，施用至少100mmol / l头孢菌素核，以3-5倍摩尔比施加游离乙酸衍生物，根据从最初pH 7.5-6.25至 pH 6.25-5.0并调节10-40℃。
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10.发明申请NOVEL PROCESS FOR THE PREPARATION OF CEPHALOSPORINS USING ACREMONIUM CHRYSOGENUM 审中-公开使用枸杞子制备碳水化合物的新方法
公开(公告)号：WO9802567A3
公开(公告)日：1998-02-19
申请号：PCT/EP9703878
申请日：1997-07-15
Applicant: GIST BROCADES BV , BOVENBERG ROELOF ARY LANS , SCHIPPER DIRK , KERKMAN RICHARD
Inventor： BOVENBERG ROELOF ARY LANS , SCHIPPER DIRK , KERKMAN RICHARD
CPC classification number: C12P35/04 , C12N9/1029
Abstract: The present invention describes a process wherein Acremonium is used as a suitable and convenient organism for the production of N-acylated cephalosporin derivatives. In the process of the invention, a recombinant, acyltransferase-expressing Acremonium strain is cultured in the presence of a suitable acyl side chain precursor. Optionally, the acyltransferase-expressing Acremonium strain further does not express hydroxylase and/or acetyltransferase activity. The N-acylated cephalosporin derivative is recovered without contaminating α-aminoadipyl cephalosporin compounds. The thus recovered compound subsequently may be deacylated via chemical or enzymatical means.
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