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217 条记录 (耗时 0.013 秒)

    Oxidation process for preparing 3-formyl-cephem derivatives
    75.
    发明授权
    Oxidation process for preparing 3-formyl-cephem derivatives 有权
    制备3-甲酰基头孢烯衍生物的氧化方法

    公开(公告)号：US09499566B2

    公开(公告)日：2016-11-22

    申请号：US14680548

    申请日：2015-04-07

    申请人： Basilea Pharmaceutica International

    发明人： Ivan Joseph Maria Vervest

    IPC分类号： C07D501/04 ,  C07D501/34

    CPC分类号： C07D501/04 ,  C07D501/34

    摘要： The present invention relates to an improved process for oxidizing 3-hydroxy-methyl-cephem derivatives to the corresponding 3-formyl-cephem derivatives. In particular this oxidation process is for the preparation of 7-[2-(5-amino-[1,2,4]thia-diazol-3-yl)-2-hydroxyimino-acetylamino]-3-formyl-8-oxo-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid derivatives of formula (I) using a combination of a hypervalent iodine oxidizing agent of the type 10-I-3 such as bis(acetoxy)iodo-benzene (BAIB) and a catalyst such as 2,2,6,6-tetramethyl-1-piperidinyloxy (TEMPO). These compounds of formula (I) are intermediates in the synthesis of ceftobiprole.

    Method for the production of ceftobiprole medocaril
    77.
    发明授权
    Method for the production of ceftobiprole medocaril 有权
    生产头孢匹隆中间体的方法

    公开(公告)号：US09139597B2

    公开(公告)日：2015-09-22

    申请号：US13320430

    申请日：2010-05-25

    申请人： Peter Kremminger ,  Johannes Ludescher ,  Hubert Sturm

    发明人： Peter Kremminger ,  Johannes Ludescher ,  Hubert Sturm

    IPC分类号： C07D501/56 ,  C07D501/04 ,  C07D501/18

    CPC分类号： C07D501/56 ,  C07D501/04 ,  C07D501/18

    摘要： The present invention relates to a method for the production of organic compounds, in particular sodium (6R,7R)-7-[(Z)-2-(5-amino-[1,2,4]thiadiazol-3-yl)-2-hydroxyimino-acetylamino]-8-oxo-3-[(E)-(R)-1′-(5-methyl-2-oxo-[1,3]-dioxol-4-ylmethoxycarbonyl)-2-oxo-[1,3′]bipyrrolidinyl-3-ylidenemethyl]-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylate (ceftobiprole medocaril), and compounds of the general formula (1) and of the general formula (2), the compounds themselves and intermediates in the production according to the invention.

    摘要翻译： 本发明涉及一种生产有机化合物的方法，特别是（6R，7R）-7 - [（Z）-2-（5-氨基 - [1,2,4]噻二唑-3-基） -2-羟基亚氨基 - 乙酰氨基] -8-氧代-3 - [（E） - （R）-1' - （5-甲基-2-氧代 - [1,3] - 二氧杂环戊烯-4-基甲氧基羰基）-2- 氧基 - [1,3']联吡咯烷基-3-亚基甲基] -5-硫杂-1-氮杂 - 双环[4.2.0]辛-2-烯-2-羧酸酯（头孢噻肟中间体）和通式（ 1）和通式（2），本发明的生产中的化合物本身和中间体。

    Novel fluorogenic substrates for beta-lactamase gene expression
    78.
    发明申请
    Novel fluorogenic substrates for beta-lactamase gene expression 审中-公开

    公开(公告)号：US20070020715A1

    公开(公告)日：2007-01-25

    申请号：US11447691

    申请日：2006-06-05

    申请人： Roger Tsien ,  Jianghong Rao

    发明人： Roger Tsien ,  Jianghong Rao

    IPC分类号： C12Q1/34 ,  C12Q1/18 ,  C07F5/02 ,  C07D501/04

    CPC分类号： C12Q1/34 ,  C07D501/04 ,  C07F5/022 ,  C09B11/24 ,  C09B19/00 ,  C09B56/00 ,  C09B56/16

    摘要： Provided are fluorescent substrates β-lactamases and methods of using substrates having the general formulas: or in which where R1 is H or A is S, O, SO, SO2 or CH2; X is O; L is a linker; R2 is hydrogen; R3 is hydrogen; R4 is hydrogen; R5 is hydrogen; R6 is hydrogen; R7 is hydrogen; R8 is hydrogen; R9 is in which W is a hydrogen, alkyl, substituted heteroalkyl, aryl, a heteroaryl, substituted heteroaryl or a CN; and, S is an integer from 0 to 5; W′ and W″ are independently hydrogen, alkyl, substituted heteroalkyl, aryl, substituted heteroaryl, (═O) or OR10; wherein R10 is hydrogen, substituted alkyl, heteroalkyl, substituted heteroalkyl, aryl, substituted aryl, heteroaryl; or substituted heteroaryl; and, Y is a dye moiety or a quencher moiety. R is a benzyl, 2-thienylmethyl, or cyanomethyl group; R′ is selected from the group consisting of H, physiologically acceptable salts or metal, ester groups, ammonium cations, —CHR2OCO(CH2)nCH3, —CHR2OCOC(CH3)3, acylthiomethyl, acyloxy-alpha-benzyl, deltabutyrolactonyl, methoxycarbonyloxymethyl, phenyl, methylsulphinylmethyl, β-morpholinoethyl, dialkylaminoethyl, and dialkylaminocarbonyloxymethyl, in which R2 is selected from the group consisting of H and lower alkyl; A is selected from the group consisting of S, O, SO, SO2 and CH2; and Z is a donor fluorescent moiety. Also provided are methods of use of the compounds of the general formulas.

    Method for producing cephem compounds
    79.
    发明授权
    Method for producing cephem compounds 失效
    头孢烯化合物的制备方法

    公开(公告)号：US5162522A

    公开(公告)日：1992-11-10

    申请号：US691307

    申请日：1991-04-25

    申请人： Kenzo Naito ,  Yukio Ishibashi ,  Toshihiko Fujitani

    发明人： Kenzo Naito ,  Yukio Ishibashi ,  Toshihiko Fujitani

    IPC分类号： A61K31/545 ,  C07D501/04 ,  C07D501/18 ,  C07D501/24 ,  C07D501/26

    CPC分类号： C07D501/04 ,  C07D501/18 ,  C07D501/26

    摘要： A method for producing 3-(3-oxobutyryloxymethyl)-3-cepham-4-carboxylic acids which are antibiotics or intermediates for the synthesis of antibiotics, at a low temperature in a very short period of time and in good yield, characterized by reacting a 3-hydroxylmethyl-3-cephem-4-carboxylic acid with diketene in the presence of a 4-(tertiary-amino)pyridine and if necessary, when a 7-acylamino-3-(3-oxobutyryloxymethyl)-3-cephem-4-carboxylic acid is obtained, subjecting it to deacylation at the 7-position thereof.

    摘要翻译： 一种生产3-（3-氧代丁酰氧基甲基）-3-头孢烯-4-羧酸的方法，它是抗生素或用于合成抗生素的中间体，在非常短的时间内以低的温度和良好的产率，其特征在于反应 3-羟基甲基-3-头孢烯-4-羧酸与4-（叔 - 氨基）吡啶存在下的双烯酮，如果需要，当7-酰基氨基-3-（3-氧代丁酰氧基甲基）-3-头孢烯-4-羧酸 得到4-羧酸，使其在其7-位脱羟基。