合成路线:The condensation of methyl 5-methoxy-2-methylindole-3-acetate (I) with p-nitrobenzoyl chloride (II) by means of NaH in toluene gives methyl 1-(p-nItrobenzoyl)-5-methoxy-2-methylindole-3-acetate (III),which is hydrolyzed with p-toluenesulfonic acid in refluxing acetic acid yielding the corresponding free acid (IV).The reduction of (IV) with H2 over Pd/C in methanol affords 1-(p-aminobenzoyl)-5-methoxy-2-methyl indole-3-acetic acid (V) ,which is finally treated with NaNO2 and HCl in acetic acid,and with NaN3 in water.
参考文献标题:Synthesis and preliminary pharmacological data on zidometacin,a new anti-inflammatory compound
文献作者:Tricerri,S.; et al.
参考来源:Eur J Med Chem 1979,14181-183
合成路线:The condensation of methyl 5-methoxy-2-methylindole-3-acetate (I) with p-nitrobenzoyl chloride (II) by means of NaH in toluene gives methyl 1-(p-nItrobenzoyl)-5-methoxy-2-methylindole-3-acetate (III),which is hydrolyzed with p-toluenesulfonic acid in refluxing acetic acid yielding the corresponding free acid (IV).The reduction of (IV) with H2 over Pd/C in methanol affords 1-(p-aminobenzoyl)-5-methoxy-2-methyl indole-3-acetic acid (V) ,which is finally treated with NaNO2 and HCl in acetic acid,and with NaN3 in water.
参考文献标题:Zidometacin
文献作者:Blancafort,P.; Serradell,M.N.; de Angelis,L.; Castar,J.
参考来源:Drugs Fut 1979,4(11),839
产品链接: CAS No. 62851-43-8››