CAS: 82219-78-1; (6R,7R)-3-(((1,2,3-Thiadiazol-5-yl)Thio)Methyl)-7-((E)-2-(2-Aminothiazol-4-yl)-2-(Methoxyimino)Acetamido)-8-Oxo-5-Thia-1-Azabicyclo[4.2.0]Oct-2-Ene-2-Carboxylic Acid

上下游产品

(6R,7R)-7-{2-(2-Amino-Thiazol-4-yl)-2-[(Z)-Methoxyimino]-Acetylamino}-8-Oxo-3-([1,2,3]Thiadiazol-5-Ylsulfanylmethyl)-5-Thia-1-Aza-Bicyclo[4.2.0]Oct-2-Ene-2-Carboxylic Acid 2,2-Dimethyl-Propionyloxymethyl Ester 101004-04-0

📜(6R,7R)-7-{2-(2-Amino-Thiazol-4-yl)-2-[(Z)-Methoxyimino]-Acetylamino}-8-Oxo-3-([1,2,3]Thiadiazol-5-Ylsulfanylmethyl)-5-Thia-1-Aza-Bicyclo[4.2.0]oct-2-Ene-2-Carboxylic Acid 2,2-Dimethyl-Propionyloxymethyl Ester置于水体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,化学反应生成 (2R,6R,7R)-7-{2-(2-Amino-Thiazol-4-yl)-2-[(Z)-Methoxyimino]-Acetylamino}-8-Oxo-3-([1,2,3]Thiadiazol-5-Ylsulfanylmethyl)-5-Thia-1-Aza-Bicyclo[4.2.0]oct-3-Ene-2-Carboxylic Acid,头孢唑喃,(2R,6R,7R)-(Pivaloyloxy)Methyl 3-(((1,2,3-Thiadiazol-5-yl)Thio)Methyl)-7-((Z)-2-(2-Aminothiazol-4-yl)-2-(Methoxyimino)Acetamido)-8-Oxo-5-Thia-1-Azabicyclo[4.2.0]oct-3-Ene-2-Carboxylate
参考文献:口服活性头孢菌素酯的研究.二.新戊酰氧基甲基酯在磷酸盐缓冲溶液中的化学稳定性.
标题:口服活性头孢菌素酯的研究.二.新戊酰氧基甲基酯在磷酸盐缓冲溶液中的化学稳定性.
摘要:研究了头孢菌素的新戊酰氧基甲基(pom)酯在磷酸盐缓冲溶液(ph 6-8)中的降解动力学.起始δ3头孢菌素酯的降解主要通过异构化为δ2酯并随后水解为δ2酸而进行.水解为δ3酸(母体酸)非常缓慢.速率常数的分析表明,异构化速率k12大约等于δ3酯kdeg的表观降解速率,并且比δ2酯k24的水解速率慢.发现到δ2酯的异构化过程是头孢菌素酯降解的决定速率的步骤.头孢菌素的c-3位上的取代基影响降解动力学.ph值的升高促进了降解,
DOI:10.1248/cpb.37.2369

专利信息

专利号:US-5847150-A
优先权日:1996-04-24
标题 :Solid phase and combinatorial synthesis of substituted 2-methylene-2, 3-dihydrothiazoles and of arrays of substituted 2-methylene-2, 3-dihydrothiazoles
发明人：DORWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS
摘要:A solid phase method for the synthesis of a plurality of differently substituted 2-methylenethiazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 2-methylenethiazoles are prepared by acylation of a substrate-bound primary or secondary amine with cyanoacetic acid and reaction of the resulting cyanoacetamide with an isothiocyanate in the presence of a base. Alkylation with an appropriate alkyl halide under acidic conditions yields differently substituted, support-bound 2-methylene-2,3-dihydrothiazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 2-methylenethiazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

专利号:US-4959495-A
优先权日:1986-07-28
标 题 :Process for the preparation of intermediates used to produce aminothiazoloximino cephalosporins
发明人：CURRAN WILLIAM V
权利人:AMERICAN CYANAMID CO
摘要:A process is disclosed for the preparation of intermediates useful in the synthesis of aminothiazoloximino cephalosporins.

专利号:US-5066799-A
优先权日:1986-07-28
标题:Intermediates for the preparation of aminothiazoloximino cephalosporins
发明人：CURRAN WILLIAM V
权利人:AMERICAN CYANAMID CO
摘要:Intermediates useful in synthesis of aminothiazoloximino cephalosporins are disclosed, which intermediates can be radio-labelled for pharmacological evaluation.

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:US-2025002508-A1
优先权日:2020-05-05
标题 :Boronic acid derivatives and synthesis, polymorphic forms, and therapeutic uses thereof
发明人：HECKER SCOTT J; BOYER SERGE HENRI; BIO MATTHEW M; FANG YUANQING; GONZALES DE CASTRO ANGELA; LEFORT LAURENT; ZHU ZUOLIN; LINDER THOMAS
权利人:QPEX BIOPHARMA INC
摘要:Disclosed herein are antimicrobial compounds, polymorphic forms, compositions, pharmaceutical compositions, the method of use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents, for example, β-lactamase inhibitors (BLIs).