Potassium Syn-7-[2-(2-Aminothiazol-4-yl)-2-Hydroxyiminoacetamido]-3-Vinyl-3-Cephem-4-Carboxylate Dihydrate置于盐酸体系中,用 水 作为反应溶剂,化学反应 2.0H,以90%的收率获得产物头孢地尼 参考文献: Crystalline Forms Of Cefdinir Potassium[fr] Formes Cristallines De Cefdinir Potassium 标题: Crystalline Forms Of Cefdinir Potassium[fr] Formes Cristallines De Cefdinir Potassium 摘要:本发明涉及一种新颖的头孢地尼的晶体钾盐-头孢地尼钾四水合物,其制备方法,包括头孢地尼钾四水合物的制药组合物,以及使用头孢地尼钾四水合物治疗细菌感染的方法.此外,本发明还涉及头孢地尼钾二水合物和头孢地尼钾四水合物的混合物,其制备方法,包括该混合物的制药组合物,以及使用头孢地尼钾二水合物和头孢地尼钾四水合物的混合物治疗细菌感染的方法.此外,还涉及从头孢地尼钾四水合物中制备纯头孢地尼和头孢地尼钾二水合物的方法.
专利号:US-10925977-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications 发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S 权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS 摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
专利号:US-2024197774-A1 优先权日:2021-04-16 标 题:Synthesis of Antimicrobial PVP-coated Bismuth Nanoparticles 发明人:LOPEZ-RIBOT JOSE; VAZQUEZ-MUNOZ ROBERTO 权利人:UNIV TEXAS 摘要:Described herein is a facile, fast, and economical method for the synthesis of BAL-mediated PVP-BiNPs, using basic laboratory instruments and reagents readily available in most laboratories.
专利号:US-12221452-B2 优先权日:2017-10-04 标题:Synthesis of cantharidin 发明人:DAVIDSON MATTHEW GENE; EKLOV BRIAN MATTHEW; WUTS PETER; LOERTSCHER BRAD MELVIN; SCHOW STEVEN R 权利人:VERRICA PHARMACEUTICALS INC 摘要:The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In certain embodiments, the new Diels-Alder reaction involves reacting Compound (2) in the presence of furan, and in the absence of acid or increased pressure, in an aprotic polar solvent with slight warming, to yield Compound (1) in favorable yield and exo-endo ratio. In another aspect, the invention also provides a new Diels-Alder reaction between compounds of Formula (III) and furan to yield compounds of Formula (IV), which can then be transformed into cantharidin or analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions).
专利号:WO-2005100367-A1 优先权日:2004-04-13 标 题 :Intermediates useful in the synthesis of 3-(2-substituted vinyl) cephalosporins 发明人:KUMAR YATENDRA; PRASAD MOHAN; SINGH KAPTAN; PRASAD ASHOK; RICHHARIYA SANTOSH 权利人:RANBAXY LAB LTD; KUMAR YATENDRA; PRASAD MOHAN; SINGH KAPTAN; PRASAD ASHOK; RICHHARIYA SANTOSH 摘要:The present invention relates to crystalline intermediates useful in the synthesis of 3-(2-substituted vinyl) cephalosporins and processes for their preparation. In particular, the present invention relates to crystalline ylides of Formula I, processes for their preparation, and their use as an intermediate in thepreparation of 3-(2-substituted vinyl) cephalosporins.
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:EP-2030975-A1 优先权日:2007-08-06 标 题:CEFDINIR synthesis process 发明人:MANCA ANTONIO; FILIPPI MAURO; SALA BRUNO MAURIZIO; MONGUZZI RICCARDO AMBROGIO; FOGLIATO GIOVANNI 权利人:ACS DOBFAR SPA 摘要:Cefdinir preparation by synthesis of new key intermediates, isolable as variously solvated species complexed with thiophosphoric acid derivatives or with phosphoric acid derivatives.
1: Chen Z, Bi X, Li J, Tang Y, Fan G, Sun D. Application and optimization of organic-inorganic hybrid monolithic capillary electrochromatography for in vivo cefdinir determination with microdialysis. J Sep Sci. 2016 Jan;39(2):440-9. doi: 10.1002/jssc.201500817. Epub 2015 Dec 11. doi: 10.11817/j.issn.1672-7347.2015.09.006. Chinese. Chinese. doi: 10.1080/09593330.2015.1054318. Epub 2015 Jun 17. doi: 10.1089/cap.2014.0010. Epub 2014 Oct 9. 8: Kim YC, Kim IB, Noh CK, Quach HP, Yoon IS, Chow EC, Kim M, Jin HE, Cho KH, Chung SJ, Pang KS, Maeng HJ. Effects of 1α,25-dihydroxyvitamin D3 , the natural vitamin D receptor ligand, on the pharmacokinetics of cefdinir and cefadroxil, organic anion transporter substrates, in rat. J Pharm Sci. 2014 Nov;103(11):3793-805. doi: 10.1002/jps.24195. Epub 2014 Sep 29. doi: 10.1007/s11274-014-1710-4. Epub 2014 Aug 3. doi: 10.1016/B978-0-12-800173-8.00002-7. Review. doi: 10.1002/bmc.2938. Epub 2013 May 28. doi: 10.3109/03639045.2012.728231. doi: 10.4103/0975-7406.120080. 14: Roath MC, Di Palma JA. Correspondence: cefdinir and red stool. Gastroenterol Hepatol (N Y). 2013 Jun;9(6):338.
合成参考文献
摘要:Tested as SID 103241607 in AID 781330: https://pubchem.ncbi.nlm.nih.gov/bioassay/781330#sid=103241607