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1. 发明申请

WO2014072843A1 PROCESS FOR PREPARING ISOXAZOLYL PENICILLINS 审中-公开
标题翻译：制备ISOXAZOLYL PENICILLINS的方法
公开(公告)号：WO2014072843A1
公开(公告)日：2014-05-15
申请号：PCT/IB2013/056613
申请日：2013-08-13
申请人： VARDHMAN CHEMTECH LIMITED , GUJRAL, Rajinder Singh
发明人： GUJRAL, Rajinder Singh
IPC分类号： C07D499/16 , C07D499/12 , C07D499/76 , A61P31/04
CPC分类号： C07D499/12 , C07D499/16 , C07D499/76 , Y02P20/582
摘要： The present invention relates to a process for the preparation of isoxazolyl penicillins from sugarcane juice. The invention focuses on in-situ synthesis of isoxazolyl penicillins without isolation of the intermediates like Penicillin G and 6-APA from the reaction sequence.
摘要翻译：本发明涉及从甘蔗汁制备异恶唑青霉素的方法。本发明专注于异构恶唑青霉素的原位合成，而不从反应顺序分离中间体如青霉素G和6-APA。

2. 发明申请

WO2009016170A1 PROCESS FOR THE SILYLATION OF BETA-LACTAM COMPOUNDS 审中-公开
标题翻译： BETA-LACTAM化合物的硅烷化方法
公开(公告)号：WO2009016170A1
公开(公告)日：2009-02-05
申请号：PCT/EP2008/059919
申请日：2008-07-29
申请人： DSM IP Assets B.V. , PLUGGE, Willem , KUIPERS, Karel Hendrik , VAN DER ZALM, Johannes Albert
发明人： PLUGGE, Willem , KUIPERS, Karel Hendrik , VAN DER ZALM, Johannes Albert
IPC分类号： C07F7/18 , C07D499/12 , C07D501/06
CPC分类号： C07F7/188
摘要： The present invention relates to a process for the silylation of a β-lactam compound in an organic solvent comprising one or more silylating agents characterized in that the process is carried out in the presence of an effective amount of ammonium chloride and/or the HCI salt of an organic amine.
摘要翻译：本发明涉及在含有一种或多种甲硅烷基化剂的有机溶剂中甲硅烷基化β-内酰胺化合物的方法，其特征在于该方法在有效量的氯化铵和/或HCl盐的存在下进行的有机胺。

3. 发明申请

WO2012164355A1 IMPROVED PROCESS FOR PREPARING PENICILLINS AND INTERMEDIATE COMPOUNDS 审中-公开
标题翻译：制备泼尼松和中间体化合物的改进方法
公开(公告)号：WO2012164355A1
公开(公告)日：2012-12-06
申请号：PCT/IB2011/053131
申请日：2011-07-13
申请人： VARDHMAN CHEMTECH LIMITED , GUJRAL, Rajinder Singh , JAIN, Suyog
发明人： GUJRAL, Rajinder Singh , JAIN, Suyog
IPC分类号： C07D499/12 , C07D499/76
CPC分类号： C07D499/76 , C07D499/12
摘要： Disclosed is an improved process for the preparation of isoxazolyl penicillins of formula (I), wherein X 1 and X 2 can be independently selected from the group comprising hydrogen, chlorine or fluorine, and its pharmaceutically suitable salts. The process is economic in -situ synthetic method without isolation of any intermediate. (I).
摘要翻译：公开了制备式（I）的异恶唑青霉素的改进方法，其中X 1和X 2可以独立地选自氢，氯或氟及其药学上合适的盐。该方法是经济的，而不分离任何中间体。（一世）。

4. 发明申请

WO2016139373A1 TETRAKIS(DIMETHOXYPHENYL)ADAMANTANE (TDA) AND ITS INCLUSION COMPLEXES 审中-公开
标题翻译：四氯乙烯（二甲氧基苯基）亚胺（TDA）及其包合物
公开(公告)号：WO2016139373A1
公开(公告)日：2016-09-09
申请号：PCT/EP2016/054833
申请日：2016-03-07
申请人： RICHERT, Clemens , FREY, Wolfgang , SCHWENGER, Alexander
发明人： RICHERT, Clemens , FREY, Wolfgang , SCHWENGER, Alexander
IPC分类号： C07C43/21 , B01J20/22 , C07C31/08 , C07C31/10 , C07C31/125 , C07C205/02 , C07C205/06 , C07C211/46 , C07C49/08 , C07D499/12 , C07C255/03 , C07C9/15 , C07C13/18 , C07D295/192 , C07C15/04 , C07C19/03 , C07C19/04 , C07C25/13
CPC分类号： C07C43/21 , B01D53/02 , B01D2253/20 , B01D2253/25 , B01D2257/2064 , B01D2257/40 , B01D2257/7027 , B01J20/22 , B01J20/3253 , C07C9/15 , C07C13/18 , C07C15/04 , C07C31/08 , C07C31/10 , C07C31/125 , C07C49/08 , C07C205/02 , C07C205/06 , C07C255/03 , C07C2601/14 , C07C2603/74 , C07D295/192 , C07D499/12 , Y02P20/154
摘要： Molecular storage materials for incorporating small molecules in solid matrices may find applications in structure elucidation, decontamination, and slow release of active ingredients. The syntheses of 1,3,5,7-tetrakis(2,4-dimethoxyphenyl)adamantane (TDA), 1,3,5,7-tetrakis(4-methoxyphenyl)adamantane, 1,3,5,7-tetrakis(4-methoxy-2-methylphenyl)adamantane, and 1,3,5,7-tetrakis(4-methoxy-2-ethylphenyl)adamantane are reported, together with details on their X-ray crystal structures. All four adamantanes crystallize readily. The octaether shows an unusual level of pseudopolymorphism in the solid state,and includes a wide range of different guest molecules in its crystal lattices. Thus far, 20 different inclusion complexes with guest molecules ranging from methanol or trifluorobenzene were characterized. Both nitromethane and benzene were taken up into inclusion materials and were shown to be released by one of three different processes.
摘要翻译：用于在固体基质中引入小分子的分子存储材料可用于结构阐明，去污和活性成分的缓释。 1,3,5,7-四（2,4-二甲氧基苯基）金刚烷（TDA），1,3,5,7-四（4-甲氧基苯基）金刚烷，1,3,5,7-四（ 4-甲氧基-2-甲基苯基）金刚烷和1,3,5,7-四（4-甲氧基-2-乙基苯基）金刚烷及其X射线晶体结构的细节。所有四种金刚烷都容易结晶。八面体在固态中显示出异常的假多晶型水平，并且在其晶格中包括大范围的不同客体分子。到目前为止，表征了与甲醇或三氟苯的客体分子的20种不同的包合配合物。硝基甲烷和苯都被纳入包含物质中，并被证明是通过三种不同方法之一释放出来的。

5. 发明申请

WO01030783A1 PROCESS FOR THE PREPARATION OF A beta -LACTAM ANTIBIOTIC 审中-公开
标题翻译：制备β-LACTAM抗生素的方法
公开(公告)号：WO01030783A1
公开(公告)日：2001-05-03
申请号：PCT/NL2000/000636
申请日：2000-09-08
IPC分类号： C07D499/00 , C07D499/12 , C07D501/00 , C07D501/06
CPC分类号： C07D499/00 , C07D501/00
摘要： Process for the preparation of a beta -lactam antibiotic by acylation of a beta -lactam nucleus with the aid of an acylating agent, use being made of a complexing agent, and the acylating agent containing L-isomer and an aldehyde being added during the preparation. This process makes it possible to use a racemic mixture as acylating agent in the preparation of a beta -lactam antibiotic.
摘要翻译：借助于酰化剂，通过使用络合剂制备β-内酰胺抗原细胞制备β-内酰胺抗体的方法，并且在制备过程中加入含有L-异构体和醛的酰化剂。该方法可以使用外消旋混合物作为制备β-内酰胺抗生素的酰化剂。

6. 发明申请

WO99055709A1 PREPARATION OF beta -LACTAM ANTIBIOTICS IN THE PRESENCE OF UREA OR AMIDE 审中-公开
标题翻译：在尿素或其他药物存在下制备β-LACTAM抗生素
公开(公告)号：WO99055709A1
公开(公告)日：1999-11-04
申请号：PCT/NL1999/000247
申请日：1999-04-27
IPC分类号： C07D499/00 , C07D499/12 , C07D501/00 , C07D501/06
CPC分类号： C07D501/00 , C07D499/00
摘要： A process to prepare a crystalline beta -lactam compound by the addition of a base to an acidic solution of a beta -lactam compound obtained by the addition of an acid to a solution or suspension of a beta -lactam compound obtained by (a) an acylation reaction of 6-amino-penicillanic acid, 7-amino-cephalosporanic acid, 7-amino-3'-desacetoxycephalosporanic acid or 3-chloro-7-aminodesacetoxydesmethylcephalosporanic acid or derivatives thereof with a mixed-anhydride of the Dane salt of any one of the compound comprising D-phenyl-glycine, D-p-hydroxyphenyl-glycine, D-2(1,4-cyclohexadien-1-yl)glycine or (2-aminothiazol-4-yl)-(2-methoxy-imino-acetic acid) in one or more organic solvents, or (b) dissolving or suspending a crude beta -lactam compound in a solution comprising water and/or one or more organic solvents, wherein, to the solution or suspension of a beta -lactam compound, urea or derivatives thereof and/or amide or derivatives thereof are added.
摘要翻译：通过向通过（a）得到的β-内酰胺化合物的溶液或悬浮液中加入通过将酸加成获得的β-内酰胺化合物的酸性溶液中加入碱来制备结晶β-内酰胺化合物的方法 6-氨基 - 青霉烷酸，7-氨基 - 头孢烷酸，7-氨基-3'-脱乙酰氧基头孢烷酸或3-氯-7-氨基脱乙酸基甲基头孢烷酸或其衍生物与任何一种的丹烷盐的混合酐的酰化反应包括D-苯基 - 甘氨酸，Dp-羟基苯基 - 甘氨酸，D-2（1,4-环己二烯-1-基）甘氨酸或（2-氨基噻唑-4-基） - （2-甲氧基 - 亚氨基 - 乙酸酸），或（b）将粗制β-内酰胺化合物溶解或悬浮在包含水和/或一种或多种有机溶剂的溶液中，其中向β-内酰胺化合物的溶液或悬浮液中，加入脲或其衍生物和/或其酰胺或其衍生物。

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