CAS: 51940-44-4; 8-Ethyl-5-Oxo-2-(Piperazin-1-yl)-5,8-Dihydropyrido[2,3-D]Pyrimidine-6-Carboxylic Acid

该化合物是一种属于五醇类的合成抗微生物剂,主要用作治疗尿道感染的抗生素;该化合物展示了对各种克型阴性细菌和一些克型阳性细菌的广泛频谱活动,抑制细菌DNA晶体酶和四类异构酶,这是DNA复制和转录所必不可少的;Pipemidic酸的特点是水溶性相对较低,可影响其生物利用率和药用动力学;该物质一般是口服的,以其有利的安全特征著称,尽管它可能造成副作用,例如胃肠扰动或某些人过敏反应;其化学结构包括管状环,有助于其药理特性;与许多抗药剂一样,抗药的出现令人关切,需要临床环境中谨慎使用和监测;

结构式图片

欧盟法规

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CAS号142-63-2 哌嗪(六水) | CAS号19572-11-3 2-Methylmercapt... | CAS号64-67-5 硫酸二乙酯

合成工艺路线路线简述

  • 合成目标产物 Pipemidic Acid 主要起始原料 Ethyl 8-Ethyl-5-Oxo-2-(Piperazin-1-
  • (文献来源)合成步骤主要原料 Ethyl 8-Ethyl-5-Oxo-2-(Piperazin-1-
2-(4-Acetyl-Piperazin-1-yl)-8-Ethyl-5-Oxo-5,8-Dihydro-Pyrido[2,3-D]Pyrimidine-6-Carboxylic Acid Ethyl Ester置于sodium Hydroxide体系中,化学反应生成 吡哌酸
参考文献:Antibacterial Pharmaceutical Compositions And Processes For Preparation
标题:Antibacterial Pharmaceutical Compositions And Processes For Preparation
摘要:该发明提供了以下结构的化合物 ##spc1## 其中r.Sub.1是氢原子,具有1至4个碳原子的烷基基团,具有2至4个碳原子的羟基烷基基团,苄基,被甲氧基取代的苄基,苯基,丙炔基或酰基;r.Sub.2是氢原子,具有1至4个碳原子的烷基基团,被羟基或卤素取代的具有2至4个碳原子的烷基基团,乙烯基,烯丙基或苄基;r.Sub.3是氢原子或具有1至6个碳原子的烷基基团;及其盐,以及其制备方法.其中一些化合物具有抗菌活性.

海关参考信息

专利信息


专利号:WO-2004113530-A1
优先权日:2003-06-18
标题:Polynucleotide for synthesis of labeled protein
发明人:NAKA DAIJI; NAKANO HIROSHI; SHIRATORI MIWA; KOBAYASHI TERUAKI; SUZUKI KATSUHIKO; HASHIMOTO HIDEMI; SASAKI TOORU
权利人:MITSUBISHI CHEM CORP; NAKA DAIJI; NAKANO HIROSHI; SHIRATORI MIWA; KOBAYASHI TERUAKI; SUZUKI KATSUHIKO; HASHIMOTO HIDEMI; SASAKI TOORU
摘要:A process for producing a labeled protein, comprising translating a gene template in the presence of a labeled compound having a label portion consisting of a labeled substance and an acceptor portion consisting of a compound capable of binding to the C-terminus of protein synthesized by a translation system. In particular, there are provided a polynucleotide for use in synthesis of labeled protein characterized by having the capability of enhancing labeling efficiency through addition to the 3’ end of a base sequence coding for target protein within the gene template and provided a process for producing a labeled protein that is carried out with the use of the polynucleotide.

专利号:US-11332444-B2
优先权日:2018-04-25
标题:Method for the hydrolysis of quinolonecarboxylic esters
发明人:FEY PETER; BERWE MATHIAS; WIRTHS Joerg; WISCHNAT RALF; LONGERICH MARKUS; DIETZEL ANTJE
权利人:BAYER ANIMAL HEALTH GMBH
摘要:Quinolonecarboxylic esters of the general formula (II) are hydrolyzed to quinolonecarboxylic acids of the general formula (I):The method comprises the step A):A) reacting compounds of the formula (II) with a mixture comprising acetic acid, sulfuric acid and waterIn step A), ≥30 to ≤40 mol of acetic acid, ≥0.3 to ≤1 mol of sulfuric acid and ≥0.9 to ≤2.5 mol of water are used per mole of compounds of the formula (II). The method is particularly suitable for the synthesis of the intermediate (I) in the synthesis of pradofloxacin.

专利号:US-8017776-B2
优先权日:2003-07-15
标题 :Methods for synthesis of acyloxyalkyl compounds
发明人:BHAT LAXMINARAYAN; GALLOP MARK A
权利人:XENOPORT INC
摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.

专利号:US-8143437-B2
优先权日:2002-02-19
标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
发明人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X
权利人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X; XENOPORT INC
摘要:The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.

专利号:US-2010203587-A1
优先权日:2009-01-13
标 题:Use of dna gyrase inhibitors for in vitro polypeptide synthesis reactions
发明人:VOLOSHIN ALEXEI M; ZAWADA JAMES F; GOLD DANIEL
权利人:SUTRO BIOPHARMA INC
摘要:The present invention provides methods and compositions useful for in vitro polypeptide synthesis reactions. The methods involve the use of DNA gyrase inhibitors to prevent bacterial contamination in lysates used for in vitro production of polypeptides. The compositions include contamination-free cell lysates for in vitro protein synthesis reactions.

专利号:US-2003180254-A1
优先权日:1995-05-26
标题:Immunologic enhancement with intermittent interleukin-2 therapy
发明人:LANE H CLIFFORD; KOVACS JOSEPH A; FAUCI ANTHONY S
权利人:GOVT OF THE USA AS REPRESENTED
摘要:A method for activating a mammalian immune system entails a series of IL-2 administrations that are effected intermittently over an extended period. Each administration of IL-2 is sufficient to allow spontaneous DNA synthesis in peripheral blood or lymph node cells of the patient to increase and peak, and each subsequent administration follows the preceding administration in the series by a period of time that is sufficient to allow IL-2 receptor expression in peripheral or lymph node blood of the patient to increase, peak and then decrease to 50% of peak value. This intermittent IL-2 therapy can be combined with another therapy which targets a specific disease state, such as an anti-retroviral therapy comprising, for example, the administration of AZT, ddI or interferon alpha. In addition, IL-2 administration can be employed to facilitate in situ transduction of T cells in the context of gene therapy. By this approach the cells are first activated in vivo via the aforementioned IL-2 therapy, and transduction then is effected by delivering a genetically engineered retroviral vector directly to the patient.
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主要参考文献


1: Sharma V, Das R, Mehta DK, Sharma D. Novel quinolone substituted 1,3,4-oxadiazole derivatives: design, synthesis, antimicrobial and anti- inflammatory potential. Mol Divers. 2024 Aug 3. doi: 10.1007/s11030-024-10949-y. Epub ahead of print.
190:106611. doi: 10.1016/j.micpath.2024.106611. Epub 2024 Mar 11. 39(7):1143-1149. doi: 10.1007/s44211-023-00323-7. Epub 2023 Mar 23. 57(1):214-221. doi: 10.1021/acs.est.2c05963. Epub 2022 Dec 5. 77(12):3270-3274. doi: 10.1093/jac/dkac312.
311:119921. doi: 10.1016/j.envpol.2022.119921. Epub 2022 Aug 13.

合成参考文献


摘要:S10 | SWISSPHARMA | Pharmaceutical List with Consumption Data | DOI:10.5281/zenodo.2623484
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