公开(公告)号：EP2006290A4

公开(公告)日：2011-01-05

申请号：EP07739783

申请日：2007-03-27

申请人： KANEKA CORP

发明人： NISHINO KEITA ,  KOGA TERUYOSHI

IPC分类号： C07D477/00 ,  C07D477/08 ,  C07D487/04

CPC分类号： C07D477/08

公开(公告)号：EP1201665A4

公开(公告)日：2002-10-23

申请号：EP00948257

申请日：2000-07-27

申请人： EISAI CO LTD

发明人： KAYANO AKIO ,  CHIBA HIROYUKI ,  NAKAMURA TAIJU ,  SAKURAI SHIN ,  ISHIZUKA HIROYUKI ,  SAITO HIROYUKI ,  KOMATSU YUUKI ,  SASHO MANABU ,  SATO NOBUAKI ,  NEGI SHIGETO

IPC分类号： C07D477/02 ,  C07D477/08 ,  C07D477/20 ,  C07D499/68 ,  C07D501/22 ,  C07D501/36 ,  C07D501/46 ,  C07D463/00 ,  C07D499/00 ,  C07D501/00

CPC分类号： C07D477/20 ,  C07D477/02 ,  C07D477/08 ,  Y02P20/55

摘要： An industrially excellent novel process for the preparation of addition salts of basic antibiotics with inorganic acids (such as hydrochloric acid), by subjecting a basic antibiotic-oxalic acid addition salt (II) to salt-exchange with an inorganic acid salt (III) of an alkaline earth metal, wherein A is a basic antibiotic; R10 is a protected functional group to be used in organic synthesis; Ak-E is an alkaline earth metal; and B is an inorganic acid; carbapenem derivative-oxalic acid addition salts represented by general formula (II-I) and being useful as intermediates for the preparation of hydrochlorides of antimicrobial agents; and a process for preparing the same, (II-I) wherein A is a three- to seven-membered ring having at least one nitrogen atom; R1 is hydrogen or the like; R?2 and R5¿ are each hydrogen or a protecting group; R3 is a protecting group; R4 is hydrogen or the like; and R6 is hydrogen or the like.

公开(公告)号：EP0912576B1

公开(公告)日：2001-12-12

申请号：EP97934060.1

申请日：1997-07-08

申请人： MERCK & CO., INC.

发明人： WILLIAMS, John, M. ,  JOBSON, Ronald, B.

IPC分类号： C07D477/08

CPC分类号： C07D477/20 ,  C07D477/02 ,  Y02P20/55

摘要： A process for synthesizing a coumpond of formula (I) or a pharmaceutically acceptable salt or ester thereof, wherein each P independently represents H or a protecting group, and R?1 and R2¿ independently represent H, C¿1-10? alkyl, aryl or heteroaryl, or substituted C1-10 alkyl, aryl or heteroaryl, comprising: reacting the compounds (II) or a pharmaceutically acceptable salt or ester thereof, and (III) or a pharmaceutically acceptable salt or ester thereof, wherein X represents OP(O)(OR)2, or OSO2R, wherein R represents C1-6 alkyl, aryl or perfluoro C1-6 alkyl, in the presence of an amine selected from the group consisting of: diisopropylamine (DIPA), dicyclohexylamine (DCHA), 2,2,6,6-tetramethylpiperidine (TMP), 1,1,3,3-tetramethylguanidine (TMG), 1,8-diazabicyclo[4.3.0]undec-7-ene (DBU) and 1,5-diazabicyclo[4.3.0]non-5-ene to produce a compound of formula (I).

公开(公告)号：EP3269718A1

公开(公告)日：2018-01-17

申请号：EP16178957.3

申请日：2016-07-12

申请人： Evonik Degussa GmbH

发明人： GRÜNEWALD, Elena ,  WEIDLICH, Stephan ,  JANTKE, Ralf

IPC分类号： C07D477/08 ,  C07D477/20 ,  A61K31/407 ,  A61K31/04

CPC分类号： C07D477/08 ,  C07D477/20 ,  Y02P20/55

摘要： Verfahren zur Herstellung eines Carbapenems oder dessen Vorstufe (I) durch Abspaltung einer oder mehrerer Schutzgruppen einer Substanz (II).

enthaltend die Schritte:
a) Hydrierung mit Wasserstoff eines Reaktionsgemisches (1) enthaltend die Substanz (II), mindestens ein organisches Lösungsmittel und mindestens ein aromatisches Amin in Gegenwart eines heterogenen Hydrierkatalysators unter Bildung eines Produktgemisches (1),
b) Abtrennung des heterogenen Katalysators aus dem Produktgemisch (1) unter Bildung eines Produktgemisches (2),
c) Hinzufügen von Wasser zum Produktgemisch (2), wobei das Gewichtsverhältnis von zugegebenem Wasser zum Produktgemisch (2) von 0,1 bis 10 ist,
d) Thermische Behandlung des Produktgemisches (II) unter Bildung eines Produktgemisches (3) enthaltend Substanz (I).

摘要翻译： 通过裂解物质（II）的一个或多个保护基来制备碳代青霉烯或其前体（I）的方法。 包括以下步骤：a）用反应混合物的氢氢化（1）含有在非均相氢化催化剂的存在下，物质（II），至少一种有机溶剂和至少一种芳族胺反应形成的产物混合物（1），b）将非均相催化剂从分离 c）向产物混合物（2）中加入水，加入的水与产物混合物（2）的重量比为0.1-10，d）产物混合物（1）的热处理， II）以形成含有物质（I）的产物混合物（3）。

公开(公告)号：EP1426376A1

公开(公告)日：2004-06-09

申请号：EP02755773.5

申请日：2002-08-02

申请人： Eisai Co., Ltd.

发明人： TSUJII, Masahiko ,  ISHIZUKA, Hiroyuki ,  KOIWA, Atsushi

IPC分类号： C07D477/06 ,  C07D477/08

CPC分类号： C07D477/20 ,  C07D477/02 ,  Y02P20/55

摘要： A process for the preparation of carbapenem antibiotics, which is free from the two disadvantages: (1) use of column chromatography and (2) recovery of a difficulty soluble salt and by which the objective compounds can be efficiently prepared in a short period. Specifically, a process for the preparation of compounds represented by the general formula (IV), salts thereof, or hydrates of both, characterized by reacting a compound represented by the general formula (I) with a compound represented by the general formula (II): X-H (wherein X is a member selected from the group consisting of substituents represented by the formulae (X-1) to (X-8)) to thereby obtain a compound represented by the general formula (III) or salt thereof, converting the compound (III) or salt thereof into a compound represented by the general formula (IV) or a salt thereof through the removal of the protecting group (R3), and purifying the compound (IV) or salt thereof by crystallization.

摘要翻译： 制备碳青霉烯类抗生素的方法没有两个缺点：（1）使用柱色谱和（2）难以溶解的盐的回收，并且可以在短时间内有效地制备目标化合物。 具体而言，制备由通式（IV）表示的化合物，其盐或两者的水合物的方法，其特征在于使由通式（I）表示的化合物与由通式（II）表示的化合物反应， ：XH（其中X是选自由式（X-1）至（X-8）表示的取代基组成的组中的成员），由此获得由通式（III）表示的化合物或其盐， 化合物（Ⅲ）或其盐通过除去保护基（R3）而转化为通式（Ⅳ）代表的化合物或其盐，并通过结晶纯化化合物（Ⅳ）或其盐。

公开(公告)号：EP2906561A1

公开(公告)日：2015-08-19

申请号：EP13774444.7

申请日：2013-10-11

申请人： Sandoz AG

发明人： LENGAUER, Hannes ,  ENDL, Birgit ,  FELZMANN, Wolfgang

IPC分类号： C07D477/08 ,  C07D477/20

CPC分类号： C07D477/08 ,  C07B2200/13 ,  C07D477/20

摘要： The present invention relates to the preparation of compounds, in particular to the preparation of compounds which may be used as intermediates for the preparation of antibiotics, preferably carbapenem antibiotics, more preferably ertapenem, and salts thereof.

摘要翻译： 本发明涉及化合物的制备，特别是制备可用作制备抗生素，优选碳青霉烯类抗生素，更优选厄来替班及其盐的中间体的化合物。

公开(公告)号：EP1426376A4

公开(公告)日：2004-12-22

申请号：EP02755773

申请日：2002-08-02

申请人： EISAI CO LTD

发明人： TSUJII MASAHIKO ,  ISHIZUKA HIROYUKI ,  KOIWA ATSUSHI

IPC分类号： A61P31/04 ,  C07D477/02 ,  C07D477/20 ,  C07D477/06 ,  A61K31/407 ,  C07D477/08

CPC分类号： C07D477/20 ,  C07D477/02 ,  Y02P20/55

摘要： A process for the preparation of carbapenem antibiotics, which is freed from the two disadvantages: (1) use of column chromatography and (2) recovery of a difficultly soluble salt and by which the objective compounds can be efficiently prepared in a short period. Specifically, a process for the preparation of compounds represented by the general formula (IV), salts thereof, or hydrates of both, characterized by reacting a compound represented by the general formula (I) with a compound represented by the general formula (II): X - H (wherein X is a member selected from the group consisting of substituents represented by the formulae (X-1) to (X-8)) to thereby obtain a compound represented by the general formula (III) or a salt thereof, converting the compound (III) or salt thereof into a compound represented by the general formula (IV) or a salt thereof through the removal of the protective group (R3), and purifying the compounds (IV) or salt thereof by crystallization. (I) (X-1) (X-2) (X-3) (X-4) (X-5) (X-6) (X-7) (X-8) (III) (IV)

公开(公告)号：EP1019405A1

公开(公告)日：2000-07-19

申请号：EP96940727.9

申请日：1996-12-04

申请人： Korea Research Institute of Chemical Technology

发明人： LEE, Cheol, Hae ,  LEE, Dong, Ha ,  KIM, Kyung, Sook ,  KIM, Jae, Hak ,  KIM, Young, Sook ,  JUN, Yu, Sung ,  LIM, Sung, Su ,  BAE, Eun, Mi ,  KIM, Bong, Jin

IPC分类号： C07D477/00 ,  C07D477/06 ,  C07D477/08 ,  A61K31/40

CPC分类号： C07D477/14

摘要： A β-methylcarbapenem compound of formula (I), a salt or an ester thereof, a process for the preparation thereof and a pharmaceutical composition containing same, wherein R1 is a C¿1-16? alkyl, C1-16 alkenyl, cycloalkyl, aryl or heterocyclic aryl group.