CAS: 189279-58-1; 1-(6-Amino-3,5-Difluoropyridin-2-yl)-8-Chloro-6-Fluoro-7-(3-Hydroxyazetidin-1-yl)-4-Oxo-1,4-Dihydroquinoline-3-Carboxylic Acid

上下游产品

CAS号120-94-5 1-甲基吡咯烷 | CAS号189279-53-6 1-(6-amino-3,5-... | CAS号189281-08-1 ethyl 5-amino-1... | CAS号18621-18-6 3-羟基氮杂环丁烷盐酸盐 | CAS号446-17-3 2,4,5-三氟苯甲酸 | CAS号88419-56-1 2,4,5-三氟苯甲酰氯 | CAS号98349-24-7 2,4,5-三氟苯甲酰乙酸乙酯

1-(6-Amino-3,5-Difluoropyridin-2-yl)-8-Chloro-6-Fluoro-7-(3-Hydroxyazetidin-1-yl)-4-Oxo-1,4-Dihydroquinoline-3-Carboxylic Acid置于sodium Hydroxide体系中,用 乙醇,水 用作溶剂,化学反应 3.0H,以94%的收率获得德拉沙星
参考文献:德拉沙星及其中间体的制备方法
标题:德拉沙星及其中间体的制备方法
摘要:本发明涉及一种抗菌药物德拉沙星及其中间体的制备方法,所述方法,步骤如下:(1)以3‑氯‑2,4,5‑氟苯甲酸(化合物1)为原料与氯化亚砜反应得到化合物2;(2)化合物2与n,N‑二甲氨基丙烯酸乙酯缩合得到化合物3;(3)化合物3与3,5‑二氟‑2,6‑二氨基吡啶进行取代得到化合物4;(4)化合物4经过缚酸剂环合得到化合物5;(5)化合物5与3‑羟基氮杂环丁烷盐酸盐反应生成化合物6;(6)化合物6经过水解得到化合物7;(7)化合物7与葡甲胺成盐得到德拉沙星.

专利信息

专利号:US-2024035023-A1
优先权日:2022-06-24
标题 :Computer implemented method for engineering fluorinase enzymes for synthesis of fluorophenyl compounds
发明人：R PRAVIN KUMAR; G GLADSTONE SIGAMANI; L ROOPA; B K NAVEEN; SHETTY ANUJ J; M LIKITH
权利人:KCAT ENZYMATIC PRIVATE LTD
摘要:The present invention discloses a computer-implemented method for engineering fluorinase enzymes towards the synthesis of fluorophenyl compounds. Limited or no mechanistic details of fluorinase enzymes have hindered progress in understanding their catalytic mechanisms for synthesizing synthetic organofluorine compounds. Through a comprehensive computational screening process, specific methionine-sulfonium phenyl substrates, including [(3S)-3-amino-3-carboxypropyl][2,5-difluoro-4-(4-methoxy-2,4-dioxobutyl)phenyl]methylsulfonium, were designed and optimized using quantum chemical optimization techniques. This methodology uncovers crucial information on F— ion attack conformation and the catalytic mechanism of the substrate, leading to the formation of Methyl 3-oxo-4-(2,4,5-trifluorophenyl)butanoate. Furthermore, a protein sequence and 3D modeling-based enzyme screening process was employed to identify the most suitable enzyme for this substrate. The identified enzyme was then engineered using the mechanistic insights gained from the studies, resulting in improved substrate scope, stability and catalytic efficiency. This computer-based approach offers an efficient and precise alternative to traditional trial-and-error methods, advancing the field towards the successful synthesis fluorophenyl compounds.

专利号:US-2014315720-A1
优先权日:2012-10-24
标 题 :Polysaccharide ester microspheres and methods and articles relating thereto
发明人：FALLON DENIS G; GARRETT THOMAS S; KIZER LAWTON E; ZAZZARA KAREN L; COMBS MICHAEL T; JOHNSON RICHARD K; DEHART GARY
权利人:CELANESE ACETATE LLC
摘要:A method for producing a polysaccharide ester microsphere may include forming a polysaccharide ester product from a polysaccharide synthesis, wherein the polysaccharide ester product comprises a polysaccharide ester and a solvent; diluting the polysaccharide ester product, thereby yielding a polysaccharide ester dope; and forming a plurality of polysaccharide ester microspheres from the polysaccharide ester dope. Suitable polysaccharides may include, but are not limited to, starch, cellulose, hemicellulose, algenates, chitosan, and any combination thereof. Esters thereof may be organic esters (e.g., acetate and the like), inorganic esters (e.g., sulfonates and the like), or combinations thereof. Further, the solids conent of the polysaccharide ester dope, in some instances, may be greater than about 16 wt %.

专利号:CN-216419381-U
优先权日:2021-11-08
标题:A kind of delafloxacin intermediate synthesis reaction device