氟替卡松丙酸酯[CAS80474-14-2]合成路线图解——原料药厂家东康源.docVIP

武汉东康源氟替卡松丙酸脂 [CAS:80474-14-2]合成路线图解 核心提示：NameFluticasone propionate;FN-25;CCI-18781;Fluspiral;Flovent Diskus;Flusonal;Flovent DPI;Fluxonal;Flonase;Flunase;FlovenName Fluticasone propionate;FN-25;CCI-18781;Fluspiral;Flovent Diskus;Flusonal;Flovent DPI;Fluxonal;Flonase;Flunase;Flovent;Flixotide;Flutide;Cutivate;Flixonase Chemical Name (6alpha,11beta,16alpha,17alpha)-6,9-Difluoro-11-hydroxy-16-methyl-3-oxo-17-(1-oxopropoxy)androsta-1,4-diene-17-carbothioic acid S-(fluoromethyl) ester　　　　　　6alpha,9-Difluoro-11beta,17-dihydroxy-16alpha-methyl-3-oxoandrosta-1,4-diene-17beta-carbothioic acid S-(fluoromethyl) ester 17-propionate CAS 80474-14-2 Related CAS Formula C25H31F3O5S Structure Formula Weight 500.58202 Tel 027 E-mail:chem@ qq:2847831942 Company 武汉东康源科技有限公司 Activity/Mechanism Antiallergy/Antiasthmatic Drugs, Asthma Therapy, Atopic Dermatitis, Agents for, Chronic Obstructive Pulmonary Diseases (COPD), Treatment of, DERMATOLOGIC DRUGS, Drugs for Allergic Rhinitis, RESPIRATORY DRUGS, Treatment of Upper Respiratory Tract Disorders, Corticosteroids Syn. Route 3 Route 1 the oxidation of flumethasone (i) with oxygen and k2co3 in methanol gives 6alpha,9alpha-difluoro-11beta,17alpha-dihydroxy-16alpha-methyl-3-oxoandrosta-1,4-diene-17beta-carboxylic acid (ii), which is partially acylated with propionic anhydride in pyridine to afford the corresponding 17alpha-propionyloxy derivative (iii) . the reaction of (iii) with dimethylthiocarbamoyl chloride and triethylamine in dichloromethane gives the corresponding carbothioic acid (iv), which is esterified with bromochloromethane and sodium bicarbonate in dimethylacetamide yielding the chloromethyl carbothioate ester (v). finally, this compound is treated with agf in acetonitrile. List of intermediates No. benzyl (2s)-2-(1,3-dioxo-1,3-dihydro-2h-isoindol-2-yl)-6-hydroxy-6-methylheptanoate (i) benzyl (2s)-6-azido-2-(1,3-dioxo-1,3-dihydro-2h-isoindol-2-yl)-6-methylheptanoate (ii) 2-[(3s)-7,7-dimet