(6R)-7T-(3,5-Di-Tert-Butyl-4-Hydroxy-Benzylideneamino)-7C-Methoxy-3-(1-Methyl-1H-Tetrazol-5-Ylsulfanylmethyl)-8-Oxo-(6Rh)-5-Thia-1-Aza-Bicyclo[4.2.0]oct-2-Ene-2-Carboxylic Acid; Benzyl-Trimethyl-Ammonium Salt置于苯肼,N,N-二乙基苯胺体系中,用 1,2-二氯乙烷 作为反应溶剂,化学反应生成 头孢甲氧氰唑 参考文献:Synthesis Of 7.Alpha.-Substituted Cephalosporins. V. Novel Oxidation Procedure For Syntheses Of 7.Alpha.-Methoxycephalosporins And 6.Alpha.-Methoxypenicillins. 标题:Synthesis Of 7.Alpha.-Substituted Cephalosporins. V. Novel Oxidation Procedure For Syntheses Of 7.Alpha.-Methoxycephalosporins And 6.Alpha.-Methoxypenicillins. 摘要: DOI:10.7164/antibiotics.29.969
专利号:US-2005186197-A1 优先权日:2002-08-29 标 题:Peptide inhibitors of beta lactamases 发明人:PALZKILL TIMOTHY; HUANG WANZHI 摘要:Peptide inhibitors of β-lactamases have been identified by the synthesis of peptide arrays using synthesis SPOT technology. These peptide inhibitors of β-lactamase have activity against a broad spectrum of β-lactamases and are useful in a variety of applications.
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-4463179-A 优先权日:1980-09-02 标题 :1H-1,2,3-triazol-5-ylthio ester of N-carbobenzyloxy-p-hydroxyphenylglycine 发明人:MURAKAMI MASAHIRO; KOBAYASHI MASATERU; YAMAMOTO KIMIYO; SHIBUYA CHISEI 权利人:ASAHI CHEMICAL IND 摘要:Novel thioesters effective as acylating agents for amines or hydrazines, especially effective as active esters in synthesis of cephalosporin compounds are disclosed. The novel thioester of the present invention can be prepared by reacting a thiol or a derivative thereof with an acetic acid derivative or a reactive derivative thereof. By reacting the thioester of the present invention with a 7-aminocephalosporin derivative or a salt thereof, cephalosporin derivatives or pharmacologically acceptable salts thereof which are excellent antibiotic substances having a high antimicrobial activity can be obtained in high yield very safely.
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.
专利号:US-8399502-B2 优先权日:2008-09-17 标 题 :Analogs of indole-3-carbinol and their use as agents against infection 发明人:JONG LING; JIANG FAMING; LI GAOQUAN; MORTELMANS KRISTIEN 权利人:JONG LING; JIANG FAMING; LI GAOQUAN; MORTELMANS KRISTIEN; STANFORD RES INST INT 摘要:Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2′-diindolylmethane, 2′,3-diindolylmethane, and 3,3′-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.
1: Matsumura Y, Yamamoto M, Nagao M, Tanaka M, Takakura S, Ichiyama S. In vitro activities and detection performances of cefmetazole and flomoxef for extended-spectrum β-lactamase and plasmid-mediated AmpC β-lactamase-producing Enterobacteriaceae. Diagn Microbiol Infect Dis. 2015 Dec 11. pii: S0732-8893(15)00438-1. doi: 10.1016/j.diagmicrobio.2015.12.001. [Epub ahead of print] doi: 10.1128/AAC.00701-15. Epub 2015 Jun 22. 3: Li LH, Yen MY, Ho CC, Wu P, Wang CC, Maurya PK, Chen PS, Chen W, Hsieh WY, Chen HW. Non-cytotoxic nanomaterials enhance antimicrobial activities of cefmetazole against multidrug-resistant Neisseria gonorrhoeae. PLoS One. 2013 May 21;8(5):e64794. doi: 10.1371/journal.pone.0064794. Print 2013. 4: Doi A, Shimada T, Harada S, Iwata K, Kamiya T. The efficacy of cefmetazole against pyelonephritis caused by extended-spectrum beta-lactamase-producing Enterobacteriaceae. Int J Infect Dis. 2013 Mar;17(3):e159-63. doi: 10.1016/j.ijid.2012.09.010. Epub 2012 Nov 8. doi: 10.1186/2045-8118-8-24.
合成参考文献
参考文献:10.1136/bcr.05.2009.1873 摘要:Cheng K, Lin– T, Tsan Y, Hu S, Wang L. Pneumomediastinum as first manifestation of emphysematous pyelonephritis in a patient who is non-diabetic. BMJ Case Reports. 2009;2009():bcr0520091873. doi: 10.1136/bcr.05.2009.1873. 参考文献:10.4111/kju.2011.52.6.425 摘要:Kim CJ, Sano T, Takimoto K. Miliary tuberculosis following transrectal ultrasonography (TRUS)-guided prostate biopsy. Korean J Urol. 2011 Jun;52(6):425–7.