📜Acetyloxymethyl (5R,6S)-6-[(1R)-1-[tert-Butyl(Dimethyl)Silyl]Oxyethyl]-3-(Carbamoyloxymethyl)-7-Oxo-4-Thia-1-Azabicyclo[3.2.0]Hept-2-Ene-2-Carboxylate置于phosphate Buffer,四丁基氟化铵体系中,用 四氢呋喃,溶剂黄146 作为反应溶剂,化学反应生成 利替培南 参考文献:The Total Synthesis Of Ritipenems. Construction Of Penem Thiazoline Ring By Incorporation Of Two 2C Units Of Glycolic Acid. 标题:The Total Synthesis Of Ritipenems. Construction Of Penem Thiazoline Ring By Incorporation Of Two 2C Units Of Glycolic Acid. 摘要:Short Syntheses Of Ritipenem Acoxyl 1A And Ritipenem 1B Are Reported. The Syntheses Start From (R)-4-Acetoxy-(S)-3-[(R)-1-(T-Butyldimethylsilyloxy)Ethyl]Azetidin-2-One 3 And Are Based On The Incorporation Of Two 2C Units Obtained By Manipulation Of Glicolyc Acid 4. DOI:10.1016/s0040-4039(00)79192-1
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: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 %.
专利号:US-4508649-A 优先权日:1981-12-11 标题 :Process for preparing optically active penems 发明人:ALPEGIANI MARCO; BATTISTINI CARLO; BEDESCHI ANGELO; FRANCESCHI GIOVANNI; FOGLIO MAURIZIO; ZARINI FRANCO 权利人:ERBA FARMITALIA 摘要:Processes for the preparation of a penem derivative of formula I ##STR1## wherein n=0 or 1; R is a carboxy protecting group or H; n R 1 is hydrogen, a hydrocarbon group substituted or unsubstituted, or lower alkoxy; and n R 2 is hydrogen, C 1 -C 5 alkyl, carbamoyl N-substituted by lower alkyl or unsubstituted, or an acyl group; n and the pharmaceutically acceptable salts thereof. n These processes allow one to prepare stereospecifically only 5R derivatives, and are characterized by R 2 -introduction at a very late stage in the synthesis, thereby enabling a great number of compounds of formula I to be prepared. n Penem derivatives are useful antibacterial agents.
专利号:NZ-505979-A 优先权日:1998-06-08 标 题 :Multibinding antibacterial agents comprising 2 antibiotic or aglycone ligands, connected by a linker, capable of affecting cell wall synthesis or metabolism
专利号:CN-102268024-A 优先权日:2011-06-10 标 题 :New crystal form of biapenem and its synthesis method
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合成参考文献
参考文献:10.2165/00002018-199615020-00001 摘要:Norrby SR. Neurotoxicity of carbapenem antibacterials. Drug Saf. 1996 Aug;15(2):87–90. doi: 10.2165/00002018-199615020-00001. 参考文献:10.1093/jac/29.2.179 摘要:Lovering AM, MacGowan AP, Lewis DA, Reeves DS. Pharmacokinetics and metabolism of FCE 22101 following its administration as the oral pro-drug FCE 22891. J Antimicrob Chemother. 1992 Feb;29(2):179–85. doi: 10.1093/jac/29.2.179. 参考文献:10.1093/jac/16.3.305 摘要:Neu HC, Chin NX, Labthavikul P. The in-vitro activity of a novel penem FCE 22101 compared to other beta-lactam antibiotics. J Antimicrob Chemother. 1985 Sep;16(3):305–13. doi: 10.1093/jac/16.3.305. 摘要:Jannuzzo MG, Vaiani R, Strolin Benedetti M, Carnovali M, Cassinelli G, Corigli R. Pharmacokinetics and metabolism of FCE 22101, a new penem antibiotic. J Chemother. 1989 Jul;1(4 Suppl):511–2. 摘要:Hitzenberger G, Strolin Benedetti M, Jannuzzo MG, Silvestri S, Moro E, Frigerio E, Sassella D. Pharmacokinetics and clinical tolerability of FCE 22101, a new penem antibiotic, in healthy volunteers after a single i.m. administration. J Chemother. 1989 Jul;1(4 Suppl):513–4.