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公开(公告)号:US20160009745A1
公开(公告)日:2016-01-14
申请号:US14863982
申请日:2015-09-24
申请人: Peter Kremminger , Hubert Sturm
发明人: Peter Kremminger , Hubert Sturm
IPC分类号: C07F9/6561 , C07D501/04 , C07C51/41 , C07D417/04 , C07C303/22
CPC分类号: C07F9/65613 , C07C51/41 , C07C303/22 , C07D417/04 , C07D501/04 , C07D501/08 , C07D501/59
摘要: The present invention relates to a novel process for preparing ceftaroline fosamil via intermediates of Formulae (1), (3) or (4) of this process.
摘要翻译: 本发明涉及通过该方法的式(1),(3)或(4)的中间体制备头孢罗林粉剂的新方法。
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公开(公告)号:US09139597B2
公开(公告)日:2015-09-22
申请号:US13320430
申请日:2010-05-25
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。
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公开(公告)号:US09040539B2
公开(公告)日:2015-05-26
申请号:US13697806
申请日:2011-05-18
申请人: Michael Oberhuber , Joerg Salchenegger , Dominic De Souza , Martin Albert , Thorsten Wilhelm , Martin Langner , Hubert Sturm , Hans-Peter Spitzenstaetter
发明人: Michael Oberhuber , Joerg Salchenegger , Dominic De Souza , Martin Albert , Thorsten Wilhelm , Martin Langner , Hubert Sturm , Hans-Peter Spitzenstaetter
IPC分类号: A61K31/496 , C07D405/14 , C07D295/155 , C07D405/06
CPC分类号: C07D295/155 , C07D405/06 , C07D405/14
摘要: A process for the preparation of a chiral compound, in particular posaconazole, wherein the process comprises mixing and reacting the compounds of formula (I) Y3—NH2; of formula (IIa) 0=C═N—Y0 and/or of formula (IIb) and of formula (III) in a solvent in any order to obtain a reaction mixture containing a chiral compound of formula (IV) and/or formula (V).
摘要翻译: 一种制备手性化合物,特别是泊沙康唑的方法,其中该方法包括将式(I)Y 3 -NH 2的化合物混合并反应; 的式(IIa)0 = C = N-Y0和/或式(IIb)和式(III)的化合物在溶剂中以任何顺序获得含有式(IV)和/或式 (V)。
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公开(公告)号:US20140213784A1
公开(公告)日:2014-07-31
申请号:US14111365
申请日:2012-04-11
申请人: Hubert Sturm , Kerstin Knepper
发明人: Hubert Sturm , Kerstin Knepper
IPC分类号: C07D413/10 , C07D417/14 , C07D487/18 , C07D265/30 , C07D265/32
CPC分类号: C07D265/30 , C07D265/32 , C07D413/10 , C07D417/14 , C07D487/18
摘要: The present invention relates to methods for the preparation of a compound having the formula (X). Individual reaction steps as well as intermediates are additionally claimed.
摘要翻译: 本发明涉及制备具有式(X)的化合物的方法。 单独的反应步骤以及中间体也被要求保护。
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公开(公告)号:US20110009648A1
公开(公告)日:2011-01-13
申请号:US12223096
申请日:2007-01-22
申请人: Martin Albert , Hubert Sturm , Andreas Berger , Peter Kremminger
发明人: Martin Albert , Hubert Sturm , Andreas Berger , Peter Kremminger
IPC分类号: C07D307/87 , C07C253/30 , C07C255/59 , C07C213/08 , C07F5/02 , C07C29/38 , C07C215/20 , C07C31/38
CPC分类号: C07C255/56 , C07C215/30 , C07C255/53 , C07D307/87
摘要: This invention relates to processes and intermediates for the stereoselective alkylation of carbonyl groups. The invention in particular allows the stereoselective preparation of the antidepressant drug escitalopram. It has been found that boric or boronic acid derivatives are useful bridging elements for the attachment of a chiral group to a compound containing a carbonyl group to be alkylated. The said borates and boronates are thus useful in a process for the asymmetric alkylation of a carbonyl group in a compound containing a carbonyl group and an anchor group capable of reacting with a boric or boronic acid derivative. The asymmetric alkylation can be carried out by admixing the compound containing a carbonyl group to be alkylated and the anchor group capable of reacting with a boric or boronic acid derivative with a boric or boronic acid derivative, adding a chiral alcohol, and adding an organometallic compound. After the alkylation reaction, the borate and boronate can be easily removed by hydrolysis.
摘要翻译: 本发明涉及羰基的立体选择性烷基化方法和中间体。 本发明特别允许立体选择性制备抗抑郁药物依他普仑。 已经发现硼酸或硼酸衍生物是用于将手性基团连接到含有待烷基化羰基的化合物的有用的桥连元件。 因此,所述硼酸盐和硼酸盐可用于在含有羰基和能够与硼酸或硼酸衍生物反应的锚定基团的化合物中羰基的不对称烷基化方法。 不对称烷基化可以通过将待烷基化的羰基和能够与硼酸或硼酸衍生物反应的锚定基团与硼酸或硼酸衍生物反应,加入手性醇,并加入有机金属化合物 。 在烷基化反应之后,可以通过水解容易地除去硼酸盐和硼酸盐。
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公开(公告)号:US20100204470A1
公开(公告)日:2010-08-12
申请号:US12301620
申请日:2007-06-25
IPC分类号: C07D413/10 , C07C211/17 , C07C211/38 , C07C211/31 , C07D307/81 , C07D277/60 , C07D333/20 , C07D401/12 , C07D405/10 , C07D487/22 , C07D239/94
CPC分类号: C07C209/68 , C07C213/02 , C07D211/32 , C07D215/227 , C07D215/56 , C07D231/14 , C07D239/94 , C07D263/24 , C07D277/82 , C07D307/87 , C07D307/88 , C07D333/16 , C07D333/56 , C07D405/06 , C07D409/06 , C07D471/04 , C07D487/04 , C07C211/38 , C07C211/42 , C07C217/74
摘要: The present invention provides a new method for preparation and crystallization of hydrochlorides, hydrobromides or hydroiodides of pharmaceutical compounds or their intermediates in which the base or its acid addition salt is reacted in a solvent with a Trialkylsilylhalogenide.
摘要翻译: 本发明提供了一种用于制备和结晶药物化合物或其中间体的盐酸盐,氢溴酸盐或氢碘酸盐的新方法,其中碱或其酸加成盐在溶剂中与三烷基甲硅烷基卤化物反应。
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公开(公告)号:US06825345B2
公开(公告)日:2004-11-30
申请号:US10261748
申请日:2002-09-30
IPC分类号: C07D50122
CPC分类号: C07D501/00 , C07D277/74
摘要: A process for the purification of cefixime via a novel tert-octylamine salt of a cefixime intermediate of formula V which may be crystalline and which may be produced in a one-pot reaction from 7-amino-3-vinyl-ceph-3-em-4-carboxylic acid.
摘要翻译: 通过式V的头孢克肟中间体的新型叔辛胺盐纯化头孢克肟的方法,其可以是结晶的,并且可以在7-氨基-3-乙烯基-Ceph-3-em- 吡啶-4-羧酸。
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公开(公告)号:US06313289B1
公开(公告)日:2001-11-06
申请号:US09341542
申请日:1999-08-04
申请人: Johannes Ludescher , Ludwig Miller , Hubert Sturm , Werner Veit , Martin Decristoforo , Siegfried Wolf
发明人: Johannes Ludescher , Ludwig Miller , Hubert Sturm , Werner Veit , Martin Decristoforo , Siegfried Wolf
IPC分类号: C07D50104
CPC分类号: C07D501/00
摘要: Crystalline 2-(amninothiazol-4-yl)-2-(tert.butoxycarbonylmethoxyimino)acetic acid-S-mercapto-benzo-thiazolylester in form of an N,N-dimethylacetamide solvate; a crystalline salt of a 7-[2-(aminothiazol-4-yl)-2-(carboxymethoxyimino)acetamido]-3-vinyl-3-cephem-4-carboxylic acid with an amine of formula N(R1)(R2)(R3), wherein R1, R2, and R3 have various meanings, a crystalline sulphuric acid addition salt of a 7-[2-(2-aminothiazol-4-yl)-2-carboxymethoxyimino)acetamido]-3-vinyl-3-cephem-4-carboxylic acid; and the use of these salts in the production of cefixime, e.g. in form of a trihydrate.
摘要翻译: N,N-二甲基乙酰胺溶剂化物形式的2-(氨基噻唑-4-基)-2-(叔丁氧基羰基甲氧基亚氨基)乙酸S-巯基 - 苯并噻唑酯的结晶; 7- [2-(氨基噻唑-4-基)-2-(羧基甲氧基亚氨基)乙酰氨基] -3-乙烯基-3-头孢烯-4-羧酸与式N(R1)(R2)的胺的结晶盐, (R3),其中R1,R2和R3具有各种含义,7- [2-(2-氨基噻唑-4-基)-2-羧甲氧基亚氨基)乙酰氨基] -3-乙烯基-3 - 头孢-4-羧酸; 以及这些盐在头孢克肟的生产中的用途。 呈三水合物的形式。
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公开(公告)号:US6093813A
公开(公告)日:2000-07-25
申请号:US163660
申请日:1998-09-30
申请人: Gerd Ascher , Johannes Ludescher , Hubert Sturm , Josef Wieser
发明人: Gerd Ascher , Johannes Ludescher , Hubert Sturm , Josef Wieser
IPC分类号: C07D501/22 , C07D499/04 , C07D501/00 , C07D501/04 , C07D501/18 , C07D501/24 , C07D501/26 , C07D501/38 , C07D501/62 , C07F7/10 , C07K5/078
CPC分类号: C07K5/06139 , C07D501/00 , Y02P20/55
摘要: Cephalosporin derivatives of formula II ##STR1## wherein R.sup.a denotes hydrogen or a silyl group; R.sup.b denotes a group of formula --OR.sup.e, wherein R.sup.e denotes hydrogen or alkyl; and R.sup.c and R.sup.d together denote a bond; in free form or in salt form.
摘要翻译: 式II的头孢菌素衍生物,其中Ra表示氢或甲硅烷基; Rb表示式-OR的基团,其中Re表示氢或烷基; Rc和Rd一起表示键; 以游离形式或盐形式。
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公开(公告)号:US5856474A
公开(公告)日:1999-01-05
申请号:US732501
申请日:1996-10-23
申请人: Gerd Ascher , Johannes Ludescher , Hubert Sturm , Josef Wieser
发明人: Gerd Ascher , Johannes Ludescher , Hubert Sturm , Josef Wieser
IPC分类号: C07D501/22 , C07D499/04 , C07D501/00 , C07D501/04 , C07D501/18 , C07D501/24 , C07D501/26 , C07D501/38 , C07D501/62 , C07F7/10 , C07K5/078
CPC分类号: C07K5/06139 , C07D501/00 , Y02P20/55
摘要: Cephalosporin derivatives of formula ##STR1## wherein R.sub.1 signifies hydrogen or a silyl protecting group, processes for their production and their use as intermediate products.
摘要翻译: PCT No.PCT / EP95 / 01538 Sec。 371日期:1996年10月23日 102(e)日期1996年10月23日PCT 1994年4月24日PCT PCT。 第WO95 / 29082号公报 日期:1995年11月2日其中R1表示氢或甲硅烷基保护基的式“IMAGE”I的头孢菌素衍生物,其生产过程及其作为中间产物的用途。
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