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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;Floven.
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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-c
arboxylic 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.
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