专利号:US-7452990-B2 优先权日:2002-12-26 标题 :Intermediates for synthesis of cephalosporins and process for preparation of such intermediates 发明人:DATTA DEBASHISH; DANTU MURALIKRISHNA; MISHRA BRIJKISHORE; SHARMA POLLEPEDDI LAKSHMI NARAYANA 权利人:LUPIN LTD 摘要:A novel 4-halo-2-oxyimino-3-oxo butyric acid-N,N-dimethyl formiminium chloride chlorosulfate of formula (I) useful in the preparation of cephalosporin antibiotics n nwhereinn n X is chlorine or bromine; R is hydrogen, C 1-4 alkyl group, an easily removable hydroxyl protective group, —CH 2 COOR 5 , or —C(CH 3 ) 2 COOR 5 , wherein R 5 is hydrogen or an easily hydrolysable ester group. The compound of formula (I) is prepared by reacting 4-halo-2-oxyimino-3-oxobutyric acid of formula (IV 1 ), n nwherein X, R and R 5 are as defined above, with N,N-dimethylformiminium chloride chlorosulphate of formula (VII)n n nin an organic solvent at a temperature ranging from −30° C. to −15° C. The cephalosporins that may be prepared from the intermediate include cefdinir, cefditoren pivoxil, cefepime, cefetamet pivoxil, cefixime, cefmenoxime, cefodizime, cefoselis, cefotaxime, cefpirome, cefpodoxime proxetil, cefquinome, ceftazidime, cefteram pivoxil, ceftiofur, ceftizoxime, ceftriaxone and cefuzonam.
专利号:US-2006135761-A1 优先权日:2002-12-26 标 题 :Novel intermediates for synthesis of cephalosporins and process for preparation of such intermediates
专利号:WO-2004058695-A1 优先权日:2002-12-26 标 题 :Novel intermediates for synthesis of cephalosporins and process for preparation of such intermediates
专利号:US-6642377-B1 优先权日:1999-07-30 标 题 :Process for the preparation of basic antibiotic-inorganic acid addition salts and intermediate oxalates 发明人:KAYANO AKIO; CHIBA HIROYUKI; NAKAMURA TAIJU; SAKURAI SHIN; ISHIZUKA HIROYUKI; SAITO HIROYUKI; KOMATSU YUUKI; SASHO MANABU; SATO NOBUAKI; NEGI SHIGETO 权利人:EISAI CO LTD 摘要:A production process which comprises subjecting a basic antibiotic.oxalate (II) to salt-exchange with an alkali earth metal salt (III) of an inorganic acid:wherein the ring A means the basic antibiotic; R<10 >means a protected functional group used in organic synthesis; Ak-E means the alkali earth metal; and B means the inorganic acid, respectively.
专利号:EP-1575913-A1 优先权日:2002-12-26 标 题:Novel intermediates for synthesis of cephalosporins and process for preparation of such intermediates
专利号:CN-109053628-A 优先权日:2018-08-21 标题 :The friendly process of microwave assisting method synthesis 2-(2-Amino-4-thiazolyl)-2-methoxyiminoacetic,thiobenzothiazole ester
摘要:Smith, L. H. S.; Coote, S. C.; Procter, D. J., Science of Synthesis: Knowledge Updates, (2010) 3, 475. 参考文献:10.1159/000239089 摘要:Dagan R. Clinical trial methodology in pediatric RTI. Preface. Chemotherapy. 1992;38 Suppl 2():1. doi: 10.1159/000239089. 参考文献:10.1159/000239094 摘要:Pukander JS, Paloheimo SH, Sipilä MM. Cefetamet pivoxil in pediatric otitis media. Chemotherapy. 1992;38 Suppl 2():25–8. doi: 10.1159/000239094. 参考文献:10.1159/000239095 摘要:Paupe J, Sarbeji M, Scheinmann P, Delacourt C, Sorin M. Clinical trials on pediatric lower-respiratory-tract infection: results and comments with cefetamet pivoxil. Chemotherapy. 1992;38 Suppl 2():29–32. doi: 10.1159/000239095. 参考文献:10.1159/000239096 摘要:Ramet J, Pierard D, Vandenberghe P, De Boeck K. Comparative study of cefetamet pivoxil and penicillin V in the treatment of group A beta-hemolytic streptococcal pharyngitis. Chemotherapy. 1992;38 Suppl 2():33–7. doi: 10.1159/000239096.