CAS: 3577-01-3; Cefaloglycin

该化合物是一种半合成抗生素,属于甲状腺素类,产自真菌,它展示了广泛的抗菌活动,特别是抗克菌菌,使其在治疗各种感染方面有用;该化合物的特点是其乙状乳腺结构,因为它是其行动机制所必需的,因为它抑制了细菌细胞壁合成; 丙烯菊酯一般通过注射进行,并因其稳定性而闻名于某些乙状腺,即某些细菌对抗其他抗生素产生酶; 其药理动因涉及良好的组织渗透,允许在不同身体场所有效治疗感染; 然而,与其他抗生素一样,乙状腺素可能会产生副作用,包括过敏反应和胃肠扰动; 使用这种抗生素明智地尽量减少抗药性的发展十分重要.

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CAS号19883-41-1 D-苯甘氨酸甲酯盐酸盐 | CAS号957-68-6 7-氨基头孢烷酸 | CAS号7765-60-8 (6R)-3-acetoxym... | CAS号33125-05-2 B°C-D-苯甘氨酸 | CAS号24461-61-8 methyl (R)-amin...

合成工艺路线路线简述

    📜(6R)-3-Acetoxymethyl-7T-((R)-2-Tert-Butoxycarbonylamino-2-Phenyl-Acetylamino)-8-Oxo-(6Rh)-5-Thia-1-Aza-Bicyclo[4.2.0]oct-2-Ene-2-Carboxylic Acid 反应生成 头孢来星
    参考文献:头孢菌素类抗生素化学.七.头孢菌素的合成及一些同系物.
    标题:头孢菌素类抗生素化学.七.头孢菌素的合成及一些同系物.
    摘要:
    DOI:10.1021/jm00323A024

    海关参考信息

    专利信息


    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-3887606-A
    优先权日:1971-06-02
    标题 :Process for the preparation of DL-phenylglycine esters
    发明人:PHILLIPPS GORDON HANLEY; STEPHENSON LESLIE; COOKSEY ALBERT ROY; CLARK JOHN COLIN
    权利人:GLAXO LAB LTD
    摘要:A process for the resolution of DL-phenylglycine esters in which said ester is treated with (+)-tartaric acid in the presence of a mixture of solvents of different polarities, one of which is an alkanol having 1-4 carbon atoms, and the (+)-hermitartrate of the D-phenylglycine ester is selectively crystallised therefrom. Dphenylglycine and/or its salts may be obtained by hydrolysis of the ester thus formed. D-phenylglycine is a valuable intermediate in the synthesis of antibiotics of the penicillin and cephalosporin types. The present invention provides a relatively cheap, high yield process for the production of optically active esters of phenylglycine by way of their diastereoisomeric salts and for the production of optically active phenylglycine therefrom. Novel D-phenylglycine esters and salts are disclosed.

    专利号:US-4340672-A
    优先权日:1979-09-19
    标 题:Enzymatic synthesis of β-lactam antibacterials
    发明人:KONDO EIJI; MITSUGI TAKASHI; FUJIWARA TAMIO; MUNEYUKI RYONOSUKE
    权利人:SHIONOGI & CO
    摘要:Penicillins and cephalosporins can be synthesized by the action of an acylase on a penicillin or cephalosporin nucleus amine as substrate and an ester (I) of the following formula as the acyl source: (I) (wherein RCO is an acyl group in penicillin or cephalosporin side chains; X is a hydrogen atom, lower alkyl group or hydroxy-lower alkyl group; Y is a hydrogen atom or a lower alkyl group; and n is a positive integer). The novel acyl source (I) is also disclosed.

    专利号:US-3759898-A
    优先权日:1971-09-14
    标 题 :Synthesis of alpha-(carbo(5-indanyloxy)) benzylpenicillin
    发明人:NAKANISHI S
    权利人:PFIZER
    摘要:THE PREPARATION OF A-(CARBO(5-INDANYLOXY))BENZYLPENICILLIN VIA THE ESTERIFICATION OF A-CARBOXYPENICILLIN WITH 5-INDANOL IN THE PRESENCE OF N, N''-DICYCLOHEXYLCARBODIIMIDE IN A REACTION-INERT SOLVENT AT A PH OF 2-8.

    专利号:US-9693999-B2
    优先权日:2011-01-26
    标题:Small molecule RNase inhibitors and methods of use
    发明人:DUNMAN PAUL M; OLSON PATRICK D; CHILDERS WAYNE
    权利人:UNIV ROCHESTER; UNIV NEBRASKA; Temple University—Of the Commonwealth System of Higher Education
    摘要:Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease. Also described herein are methods of identifying compounds for treating or preventing a microbial infection.

    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.

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    主要参考文献


    1: Tune BM, Fravert D, Hsu CY. Oxidative and mitochondrial toxic effects of cephalosporin antibiotics in the kidney. A comparative study of cephaloridine and cephaloglycin. Biochem Pharmacol. 1989 Mar 1;38(5):795-802.
    8: Barbhaiya RH, Turner P. Fluorimetric assay of cephradine, cephalexin and cephaloglycin. Br J Clin Pharmacol. 1977 Aug;4(4):427-31.
    9: Tune BM, Fravert D. Mechanisms of cephalosporin nephrotoxicity: a comparison of cephaloridine and cephaloglycin. Kidney Int. 1980 Nov;18(5):591-600.

    合成参考文献


    摘要:Chemotherapy, 18(22), 1970
    摘要:Budavari, S. (ed.). The Merck Index - An Encyclopedia of Chemicals, Drugs, and Biologicals. Whitehouse Station, NJ: Merck and Co., Inc., 1996., p. 329
    摘要:Osol, A. and J.E. Hoover, et al. (eds.). Remington's Pharmaceutical Sciences. 15th ed. Easton, Pennsylvania: Mack Publishing Co., 1975., p. 1120
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