P-Nitrobenzyl (4R,5S,6S)-3-(6,7-Dihydro-5H-Pyrazolo[1,2-A][1,2,4]Triazol-8-Ium-6-Ylsulfanyl)-6-(1-Hydroxyethyl)-4-Methyl-7-Oxo-1-Azabicyclo[3.2.0]Hept-2-Ene-2-Carboxylate置于palladium On Activated Charcoal,氢气体系中,用 四氢呋喃 用作溶剂,化学反应生成比阿培南 参考文献: An Improved Process For The Preparation Of Carbapenem Antibiotic[fr] Procédé Amélioré Pour La Préparation D'Un Antibiotique Carbapenem 标题: An Improved Process For The Preparation Of Carbapenem Antibiotic[fr] Procédé Amélioré Pour La Préparation D'Un Antibiotique Carbapenem 摘要:本发明涉及一种改进的制备式(I)比阿培南的方法,具有少于25秒的重构时间.
专利号:US-11999757-B2 优先权日:2017-11-01 标 题:Synthesis of boronate ester derivatives and uses thereof 发明人:BOYER SERGE HENRI; HECKER SCOTT J; VERZIJL GERARDUS K M; HERMSEN PETRUS J 权利人:MELINTA SUBSIDIARY CORP 摘要:Disclosed herein are methods for the preparation of boronate derivatives in the synthesis of antimicrobial compounds and uses thereof. Disclosed herein includes method of making a compound of Formula (B) by reducing the ketone group of the keto-ester compound of Formula (A), and the reduction can be performed using a Ruthenium based catalyst system or using an alcohol dehydrogenase bioreduction system.
专利号:US-10669292-B2 优先权日:2014-05-05 标 题 :Synthesis of boronate salts and uses thereof 发明人:HECKER SCOTT; BOYER SERGE 权利人:REMPEX PHARMACEUTICALS INC 摘要:Disclosed herein are boronate intermediates in the synthesis of antimicrobial compounds and the use and preparation thereof. Some embodiments relate to crystalline boronate salt derivatives and their use in the synthesis of therapeutic compounds.
专利号:US-2023286915-A1 优先权日:2020-10-07 标 题 :Synthesis of pyrrole acid derivatives 发明人:WILKINSON ANDREW; COOPER LAN; ORR DAVID; FINLAYSON JONATHAN; BUNT ADAM; KIRKHAM JAMES; LYTH DAVID; BLADES KEVIN 权利人:INFEX THERAPEUTICS LTD 摘要:This invention relates to the synthesis of compounds that can be used to treat bacterial infections in combination with other antibacterial agents, and more specifically in combination with a class of antibacterial agents known as carbapenems. The compounds resulting from the novel methods of the present invention are enzyme inhibitors and more particularly are metallo-β-lactamase inhibitors.
专利号:WO-2008134923-A1 优先权日:2007-04-28 标题 :A preparation method of thiol derivative as side chain intermediate for synthesis of carbapenem derivative 发明人:CAI JIANPING; FAN ENHAI 权利人:ZHEJIANG NEXCHEM PHARMACEUTICA; CAI JIANPING; FAN ENHAI 摘要:A preparation method of thiol derivative as side chain intermediate for synthesis of carbapenem derivative. The method is starting with trans-4-hydroxy-L-proline derivative as starting material, following by one-pot method that 2-carbonyl group is protected, 4-hydroxy is protected and 2-postion is substituted to obtain 2-amide proline derivative, then 4-postion is substituted and 4-postion is hydrolyzed in the presence of base to obtain thiol side chain derivative as important intermediate for Meropenem. The present method is simple, without separating intermediates, with high yield and easy to operate and has advantages over the prior patent methods. It is suitable for industrial production.
专利号:US-8557979-B2 优先权日:2004-06-10 标题 :Carbapenem antibacterials with gram-negative activity and processes for their preparation 发明人:CHOI WOO-BAEG; KOWALIK EWA 权利人:CHOI WOO-BAEG; KOWALIK EWA; FOB SYNTHESIS INC 摘要:The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of β-methyl carbapenems which are useful as antibacterial agents.
专利号:WO-2014097257-A1 优先权日:2012-12-21 标 题:A method of preparation of (1'r,3r,4r)-4-acetoxy-3-(1'-(tert-butyldimethylsilyloxy)ethyl)-2-azetidinone, a precursor for carbapenem antibiotics synthesis 发明人:GRZESZCZYK BARBARA; STECKO SEBASTIAN; FURMAN BARTÅ?OMIEJ; CHMIELEWSKI MAREK 权利人:INST CHEMII ORGANICZNEJ PAN 摘要:The subject of the present invention is a method of preparation of (1'R,3R,4R)-4-acetoxy-3-(1'- (tert-butyl-dimethylsilyloxy)ethyl)-2-azetidinone defined by the formula (1) which is a basic chiral building block in the synthesis of carbapenem antibiotics.
1: Nakagawa Y, Suzuki K, Hirose T, Chou T, Fujisawa S, Kida M, Usuki K, Ishida Y, Taniguchi S, Kouzai Y, Tomoyasu S, Miyazaki K, Higashihara M, Ando K, Aoki S, Arai A, Akiyama N, Hatake K, Okamoto S, Dan K, Ohyashiki K, Urabe A. Erratum to: Clinical efficacy and safety of biapenem for febrile neutropenia in patients with underlying hematopoietic diseases: a multi-institutional study. J Infect Chemother. 2010 Dec 8. [Epub ahead of print] Epub 2010 Aug 11. Epub 2010 Feb 25. Epub 2009 Apr 20. 7: Kameda K, Miki M, Ikawa K, Morikawa N, Kobayashi M. [Dosing regimen rationalization of biapenem in pediatric patients: use of Monte Carlo simulation]. Jpn J Antibiot. 2009 Feb;62(1):1-8. Japanese. Epub 2009 Feb 13.
合成参考文献
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