CAS: 21080-92-2; 3-Thiophenemalonic Acid

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CAS号104554-66-7 5-Nitro-3-thiop... | CAS号37784-63-7 3-噻吩乙酸乙酯 | CAS号37784-67-1 2-(噻吩-3-基)丙二酸二乙酯 | CAS号616-44-4 3-甲基噻吩 | CAS号61857-83-8 2,2-二甲基-5-(3-噻吩... | CAS号70158-52-0 DIMETHYL 3-THIE... | CAS号821023-59-0 5,7-dichloro-6-...

2-氰基-3-噻吩基乙酸酯置于水,Sodium Hydroxide体系中,用79.6%的收率获得3-噻吩丙二酸
参考文献:一种替卡西林钠关键中间体2-(3-噻吩基)丙二酸的制备方法
标题:一种替卡西林钠关键中间体2-(3-噻吩基)丙二酸的制备方法
摘要:本发明公开了一种替卡西林钠关键中间体2‑(3‑噻吩基)丙二酸的制备方法,属于替卡西林钠关键中间体的合成技术领域.本发明的技术方案要点为:本发明的突出特点为反应条件均不存在高温,大大降低了生产的危险性,并且产品收率较高,生产步骤操作简单.

专利信息

专利号:WO-9856944-A1
优先权日:1997-06-10
标 题 :APPLICATION OF REDUCING SULPHUR COMPOUNDS DURING ENZYMATIC PREPARATION OF β-LACTAM COMPOUNDS
发明人：WILMS JOHANNES; DE VROOM ERIK
权利人:GIST BROCADES BV; WILMS JOHANNES; VROOM ERIK DE
摘要:Disclosed is a method to improve the quality of enzymatic hydrolysis or synthesis of the substituted β-lactam compounds with respect to enzyme productivity, product quality and process streamlining (prevention of the formation deposits) by the addition of reducing sulphur compounds, such as sodium sulphite or sodium metabisulphite.

专利号:US-4171439-A
优先权日:1975-04-11
标 题 :Antibacterial analogs of isocephalosporins
发明人：CONWAY TERRY T; LIM GARY M F; MENARD MARCEL
权利人:BRISTOL MYERS CO
摘要:There is described the stereoselective total synthesis of novel DELTA 2,3-1,4-morpholine-2-carboxylic acids possessing a fused beta -lactam ring in the 1,6-position and carrying a substituent cis to carbon 5 in the 7-position of the fused ring system represented by the general formula I wherein Z is halo or hydroxyl and X is acylamino. Also included in the invention are compounds of the above formula in which the carboxyl group at the 2-position is protected as by an easily cleavable ester group and salts of both the free acids and carboxyl-protected compounds. The compounds are potent antibacterial agents.

专利号:US-2009111737-A1
优先权日:1999-05-24
标题:Novel antibacterial agents
发明人：CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES
权利人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES
摘要:This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands in their monovalent (i.e., unlinked) state have the ability to bind to a an enzyme involved in cell wall biosynthesis and metabolism, a precursor used in the synthesis of the bacterial cell wall and/or the bacterial cell surface thereby interfere with the synthesis and/or metabolism of the cell wall. In particular the multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands hasn a ligand domain capable of binding to penicillin binding proteins, a transpeptidase enzyme, a substrate of a transpeptidase enzyme, a beta-lactamase enzyme, pencillinase enzyme, cephalosporinase enzyme, a transglycoslase enzyme, or a transglycosylase enzyme substrate; Preferably, the ligands are selected from the beta lactam or glycopeptide class of antibacterial agents.

专利号:US-4171438-A
优先权日:1975-07-23
标 题:0-2-Isocephem-4-carboxylic acid derivatives as antibacterial agents
发明人：DOUGLAS JAMES L; HORNING DONALD E; MORRIS LEESON R
权利人:BRISTOL MYERS CO
摘要:There is described the stereoselective total synthesis of novel DELTA 2,3-1,4-morpholine-2-carboxylic acids possessing a fused beta -lactam ring in the 1,6-position and carrying a substituent cis to carbon 5 in the 7-position of the fused ring system represented by the general formula I wherein X is acylamino and Z represents optionally substituted C1-C6 alkyl, aryl or aralkyl. Also included in the invention are compounds of the above formula in which the carboxyl group at the 2-position is protected as by an easily cleavable ester group and salts of both the free acids and carboxyl-protected compounds. The compounds are potent antibacterial agents.

专利号:WO-9729091-A1
优先权日:1996-02-09
标题:Balanol analogues
发明人：NIELSEN JOHN; LYNGSOE LARS OLE
权利人:AUDA PHARMACEUTICALS APS; NIELSEN JOHN; LYNGSOE LARS OLE
摘要:The present invention relates to a solid phase methodology for the preparation of a combinatorial library of structural analogues of the natural product balanol (ophiocordin, azepinostatin), which is a protein kinase C (PKC) and protein kinase A (PKA) inhibitor. The method comprises solid-phase synthesis of the analog variants of balanol whereby a high molecular diversity is introduced. The synthetic scheme is based on a retrosynthetic analysis of the native structure which revealed three main building blocks suitable as templates for modification. The dicarboxy-functional moiety can be immobilised to the polymer support either as the monoallyl ester or as the internal anhydride. The libraries produced by the method are especially suited for high throughput screening of potential drug candidates for the treatment of mammals, especially humans.

专利号:US-4112230-A
优先权日:1975-04-11
标题 :Δ2,3 -1,4 Morpholine-2-carboxylic acid derivatives as antibacterial agents
发明人：MENARD MARCEL; LIM GARY M F; CONWAY TERRY T
权利人:BRISTOL MYERS CO
摘要:There is described the stereoselective total synthesis of novel DELTA 2,3-1,4-morpholine-2-carboxylic acids possessing a fused beta -lactam ring in the 1,6-position and carrying a substituent cis to carbon 5 in the 7-position of the fused ring system represented by the general formula I wherein Z is halo, hydroxyl, etherified hydroxyl or hydroxyl esterified with a carboxylic acid residue or a sulfonic acid residue and X is amino, azido or acylamino. Also included in the invention are compounds of formula I in which the carboxyl group at the 2-position is protected as by an easily cleavable ester group and salts of both the free acids and carboxyl-protected compounds of formula I. The compounds of formula I are potent antibacterial agents or are of use as intermediates in the preparation of such antibacterial agents.