CAS: 65052-63-3; (6R,7R)-7-[[(2Z)-2-(2-Amino-1,3-Thiazol-4-yl)-2-Methoxyiminoacetyl]Amino]-3-Methyl-8-Oxo-5-Thia-1-Azabicyclo[4.2.0]Oct-2-Ene-2-Carboxylic Acid

上下游产品

t-butyl 7α-amino-3-methyl-3-cephem-4-carboxylate 2-(2-aminothiazol-4-yl)-2-(methoxy)iminoacetic acid Cefetamet pivoxil ethyl 2-(2-aminothiazol-4-yl)-2-(anti)-methoxyiminoacetate

📜Ae-活性酯,7-氨基去乙酰氧基头孢烷酸置于4-二甲氨基吡啶,三乙胺体系中,用 水,丙酮 作为反应溶剂,化学反应 3.5H,以98.5%的收率获得产物原料药头孢甲肟杂质3
参考文献:一种头孢他美酸的制备方法
标题:一种头孢他美酸的制备方法
摘要:本发明涉及一种头孢他美酸的制备方法,包括合成过程,脱色,吸附过程及结晶过程,通过对合成过程,脱色,吸附过程的改进,减少了杂质,提高了产品收率和纯度.本发明提供的头孢他美酸的制备方法具有反应条件温和,并且工艺稳定,适合工业规模化生产.

专利信息

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-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-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-2025228841-A1
优先权日:2024-01-12
标题 :Compositions affecting pigment production and methods for treatment of bacterial diseases
发明人：Lee Wai Yip Thomas; LO KAI YIP GEORGE
权利人:APTORUM THERAPEUTICS LTD
摘要:Provided herein are compounds, derivatives thereof, composition comprising one or more of said compounds and derivatives, and methods for prevention and/or treatment of microbial infections and/or related diseases or conditions. The present compounds and/or derivatives thereof can be represented by Formula (II):The present methods include administering to a subject an effective amount of one or more compounds of Formula (II). In one embodiment, said microbial infections are bacterial infections. More specifically, the bacterial infections are staphylococcal infections. Compositions are provided that include compounds of formula II in combination with one or more antibiotics or one or more staphyloxanthin-synthesis-inhibiting compounds.

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).

专利号:US-11135200-B2
优先权日:2014-12-20
标题:Antimicrobial drug synthesis and therapeutic compositions
发明人：GREGG JOHN MALCOLM HALL
权利人:GREGG JOHN MALCOLM HALL
摘要:This invention relates to the medical use of an antimicrobial agent, racemic Ornidazole, its (R) and (S) enantiomers, or pharmaceutically acceptable salts or esters thereof, and to methods of treatment which involve treating a subject with Ornidazole. The racemic (rac)-ornidazole, its enantiomers, or pharmaceutically acceptable salts or esters thereof, may be used in combination with other actives. The invention also relates to pharmaceutical formulations and compositions comprising (rac)-ornidazole, (R)-ornidazole, (S)-ornidazole, or pharmaceutically acceptable salts or esters thereof, and/or other actives as well as methods to stereoselectively manufacture the enantiomers.