📜(3S)-3-({(5R,6S)-6-[(1R)-1-{[tert-Butyl(Dimethyl)Silyl]Oxy}Ethyl]-2-Carboxy-7-Oxo-4-Thia-1-Azabicyclo[3.2.0]Hept-2-En-3 Yl}Sulfanyl)Tetrahydrothiophenium-1-Olate置于四丁基氟化铵体系中,用 四氢呋喃 用作溶剂,化学反应 18.0H,以72%的收率获得硫培南 参考文献:Development Of A Practical And Convergent Process For The Preparation Of Sulopenem 标题:Development Of A Practical And Convergent Process For The Preparation Of Sulopenem 摘要:Previous Synthetic Processes For The Preparation Of Sulopenem Involved Multistep Linear Sequences In Which The Chiral Sulfoxide Side Chain Was Introduced Early In The Process. This Contribution Summarizes The Development Of A Practical And Convergent Process For The Large-Scale Preparation Of 1. The Key Step In The Synthesis Involves Cyclization Of An Oxalimide Intermediate To Provide The Thiopenem Core. This Convergent Strategy Allows For Late Introduction Of The Expensive And Labile Chiral Sulfoxide Subunit. Additionally,A Regioselective Sulfur Oxidation And An Improved Deprotection Sequence Were Developed. The Latter Provides Api Of High Purity Without The Need For Recrystallization. Doi:10.1021/op300131E
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-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:WO-2009056955-A1 优先权日:2007-10-30 标题 :Amine-bearing phospholipids (abps), their synthesis and use 发明人:ZUMBUEHL ANDREAS 权利人:UNIV BASEL; ZUMBUEHL ANDREAS 摘要:Disclosed herein are amine-bearing phospholipids (ABP). The ABPs display many properties and functionalities of naturally occurring phospholipids, but also new properties and functionalities, such as the ability to polymerize while maintaining structural integrity, that may supplement or expand the functionalities of naturally occurring phospholipids.
专利号:US-9868747-B2 优先权日:2014-02-18 标题:Marinopyrrole derivatives and methods of making and using same 发明人:LI RONGSHI; SEBTI SAID; LIU YAN; QIN YONG; SONG HAO; CHENG CHUNWEI 权利人:H LEE MOFFITT CANCER CT & RES; CHONGQING ZEIN PHARMACEUTICAL CO LTD 摘要:Marinopyrrole derivatives and methods for their synthesis and use are described herein. Novel cyclic and symmetric marinopyrroles with triazole substituents having antibacterial activity against resistant bacterial strains, such as MRSA are introduced. Also provided are methods of using the compounds for treating or preventing cancer and/or microbial infections.
专利号:US-9907753-B2 优先权日:2010-03-19 标 题 :Lipid vesicle compositions and methods of use 发明人:IRVINE DARRELL J; MOON JAEHYUN 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:The invention provides delivery systems comprised of stabilized multilamellar vesicles, as well as compositions, methods of synthesis, and methods of use thereof. The stabilized multilamellar vesicles may comprise prophylactic, therapeutic and/or diagnostic agents.
专利号:US-2014315720-A1 优先权日:2012-10-24 标 题 :Polysaccharide ester microspheres and methods and articles relating thereto 发明人:FALLON DENIS G; GARRETT THOMAS S; KIZER LAWTON E; ZAZZARA KAREN L; COMBS MICHAEL T; JOHNSON RICHARD K; DEHART GARY 权利人:CELANESE ACETATE LLC 摘要:A method for producing a polysaccharide ester microsphere may include forming a polysaccharide ester product from a polysaccharide synthesis, wherein the polysaccharide ester product comprises a polysaccharide ester and a solvent; diluting the polysaccharide ester product, thereby yielding a polysaccharide ester dope; and forming a plurality of polysaccharide ester microspheres from the polysaccharide ester dope. Suitable polysaccharides may include, but are not limited to, starch, cellulose, hemicellulose, algenates, chitosan, and any combination thereof. Esters thereof may be organic esters (e.g., acetate and the like), inorganic esters (e.g., sulfonates and the like), or combinations thereof. Further, the solids conent of the polysaccharide ester dope, in some instances, may be greater than about 16 wt %.
1: Dunne MW, Aronin SI, Das AF, Akinapelli K, Breen J, Zelasky MT, Puttagunta S. A phase 3 randomized trial of sulopenem vs. ertapenem in patients with complicated intraabdominal infections. Clin Microbiol Infect. 2024 Nov 2:S1198-743X(24)00507-X. doi: 10.1016/j.cmi.2024.10.025. Epub ahead of print. 15(6):e0060924. doi: 10.1128/mbio.00609-24. Epub 2024 May 14. 3: Negatu DA, Aragaw WW, Dartois V, Dick T. A pairwise approach to revitalize β-lactams for the treatment of TB. Antimicrob Agents Chemother. 2024 May
合成参考文献
摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2026).