CAS: 70356-03-5; (6R,7R)-7-((R)-2-Amino-2-Phenylacetamido)-3-Chloro-8-Oxo-5-Thia-1-Azabicyclo[4.2.0]Oct-2-Ene-2-Carboxylic Acid Hydrate

该化合物是一种半合成的脑膜结晶剂抗生素,主要用于治疗细菌感染,其特征是针对各种克抗体和克阴性细菌的广谱活动,该化合物通常以白色为白,在水中溶解,适于口服液配方,在水中溶解; 切水合物通过抑制细菌细胞壁合成,导致细胞分解和死亡,其药理动力学包括胃肠道吸收的良性,最高等离子浓度在管理后几小时内发生; 单水分形式表明每种纤维分子都有一种水分子,可影响其稳定性和溶性; 常见的副作用可能包括胃肠扰动,过敏反应,在稀有的情况下,更严重的超敏反应. 与所有抗生素一样,必须谨慎地使用食腐素来尽量减少抗生素抗药的风险.

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R)-7t-((R)-2-amino-2-phenyl-acetylamino)-3-chloro-8-oxo-(6rH)-5-thia-1-aza-bicyclo[4.2.0]°Ct-2-ene-2-carboxylic acid 4-nitro-benzyl ester; toluene-4-sulfonate(6R)-7t-((R)-2-amino-2-phenyl-acetylamino)-3-chloro-8-oxo-(6rH)-5-thia-1-aza-bicyclo[4.2.0]°Ct-2-ene-2-carboxylic acid 4-nitro-benzyl ester; toluene-4-sulfonate (R)-phenylglycine amide °Ct-2-ene-2-carboxylic acid(6R,7R)-1-aza-3-chloro-7-amino-8-oxo-5-thiabicyclo4.2.0°Ct-2-ene-2-carboxylic acid (R)-Phenylglycine methyl ester

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    专利信息


    专利号:US-9353057-B2
    优先权日:2003-12-30
    标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
    发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
    权利人:XENOPORT INC
    摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

    专利号:US-10768157-B2
    优先权日:2015-10-20
    标 题:Materials and methods for the detection of trace amounts of substances in biological and environmental samples
    发明人:KABIR ABUZAR; FURTON KENNETH G
    权利人:KABIR ABUZAR; FURTON KENNETH G; THE FLORIDA INTERNATIONAL UNIV BOARD OF TRUSTEES
    摘要:The subject invention provides chemical compositions and synthesis strategies to create molecularly imprinted polymers (MIPs) via sol-gel processes. In a specific embodiment, the subject invention utilizes a(n) organic, inorganic, or metallic template analyte to create a hybrid organic-inorganic or inorganic three-dimensional network possessing cavities complementary to the shape, size, and functional orientation of the template molecule or ions. The subject invention further pertains to the use of the novel MIPs as selective solid phase extraction (SPE) sorbents for pre-concentration and clean-up of trace substances in biological and environmental samples. Synthesis of other molecularly imprinted polymers with environmental, pharmaceutical, chemical, clinical, toxicological, and national security implications can be conducted in accordance with the teachings of the subject invention.

    专利号:US-5824801-A
    优先权日:1996-01-19
    标 题:Process for sterospecific synthesis of keto-enol tautomeric mixture of p nitrobenzyl (1R, 6R, 7R)-7-phenoxyacetamido-3-oxo-3-cepham-4-(R/S)-carboxylate-1-oxide and p-nitrobenzyl (1R, 6R, 7R)-7-phenoxyacteamido-3-hydroxy-3-cephem-4-carboxylate-1-oxide
    发明人:GUPTA NIRANJAN LAL; SANKARAN RAMANATHAN; CHATTEJEE SUGATA; KRISHNA TUMMA HARI
    权利人:LUPIN LAB LTD
    摘要:A process for the stereospecific synthesis of keto-enol tautomeric mixture of p-nitrobenzyl (1R,6R,7R)-7-phenoxyacetamido-3-oxo-3-cepham-4-(R/S)-carboxylate-1-oxide and p-nitrobenzyl (1R,6R,7R)-7-phenoxyacetamido-3-hydroxy-3-cephem-4-carboxylate-1-oxide is described. These compounds are valuable intermediates for the synthesis of cephalosporin antibiotics e.g. cefaclor.

    专利号:US-10925977-B2
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
    发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
    权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
    摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

    专利号:US-2024197774-A1
    优先权日:2021-04-16
    标 题:Synthesis of Antimicrobial PVP-coated Bismuth Nanoparticles
    发明人:LOPEZ-RIBOT JOSE; VAZQUEZ-MUNOZ ROBERTO
    权利人:UNIV TEXAS
    摘要:Described herein is a facile, fast, and economical method for the synthesis of BAL-mediated PVP-BiNPs, using basic laboratory instruments and reagents readily available in most laboratories.

    专利号:US-8071330-B2
    优先权日:2004-12-27
    标题:Process for the synthesis of cefaclor
    发明人:MOODY HAROLD MONRO; DOOREN THEODORUS JOHANNES GODFRIED MARIA VAN
    权利人:MOODY HAROLD MONRO; DOOREN THEODORUS JOHANNES GODFRIED MARIA VAN; DSM IP ASSETS BV
    摘要:The present invention relates to a process for the synthesis of cefaclor, which process comprises reacting 7-amino-3-chloro cephalosporanic acid (7-ACCA) with D-phenylglycine in activated form (PGa) in the presence of an enzyme in a reaction mixture to form cefaclor, wherein at least part of 7-ACCA and/or PGa are added to the reaction mixture during the course of the reaction. The invention also relates to an aqueous mixture comprising an amount of cefaclor of >10 (w/w) %, an amount of 7-amino-3-chloro cephalosporanic acid of <2 (w/w) %, and an amount of D-phenyl glycine of <2 (w/w) % and a process for the recovery of cefaclor from this aqueous mixture. The invention also relates to cefaclor in crystal form having an absorbance at 400 nm (A 400 ) of less than 0.250.

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    主要参考文献


    1: Medenecka B, Jelińska A, Zajac M, Bałdyka M, Juszkiewicz K, Oszczapowicz I. Stability of the crystalline form of cefaclor monohydrate and its pharmaceutical preparations. Acta Pol Pharm. 2009 Sep-Oct;66(5):563-9. Italian. doi: 10.1007/BF02859264. doi: 10.3349/ymj.2014.55.6.1473.
    8: Thomas PW, Cammarata M, Brodbelt JS, Fast W. Covalent inhibition of New Delhi metallo-β-lactamase-1 (NDM-1) by cefaclor. Chembiochem. 2014 Nov 24;15(17):2541-8. doi: 10.1002/cbic.201402268. Epub 2014 Oct 10. doi: 10.1093/chromsci/bmt092. Epub 2013 Jul 9. doi: 10.1007/s00431-012-1926-y. Epub 2013 Jan 8. doi: 10.2478/acph-2013-0003. doi: 10.1016/j.xphs.2015.12.003. Epub 2016 Jan 30. doi: 10.1107/S0108270113026863. Epub 2013 Oct 19. Italian. doi: 10.1055/s-0031-1298012. Epub 2012 Jan 27. doi: 10.1002/jms.3510. Italian. doi: 10.1016/j.regpep.2009.11.009.

    合成参考文献


    摘要:Iyakuhin Kenkyu. Study of Medical Supplies., 13(637), 1982
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