申请人:STERLING DRUG INC.
公开号:EP0089394A1
公开(公告)日:1983-09-28
1-R,-4- or 5-[4-pyridinyl-(CH2)n]-1H-indole-2,3-dione 3-Q derivatives, useful as cardiotonics, bronchodilators, anti-asthmatics, anti-allergics and anti-cholinergics, are prepared by cyclization of an N-3- or 4-[4-pyridinyl(CH2)n]phenyl}- glyoxalamide oxime with acid; reaction of the product thus obtained with a carbonyl reactive reagent to prepare a compound where Q is other than 0; and reaction of a compound where 0 is either O or other than O with a lower-alkyl, hydroxy-lower-alkyl or di-lower-alkylamino-lower-alkyl ester of a strong mineral acid or with a carbo-lower-alkoxy-lower-alkyl halide to prepare compounds where R, is other than hydrogen.
1-R,-4-或 5-[4-吡啶基-(CH2)n]-1H-吲哚-2,3-二酮 3-Q 衍生物,可用作强心剂、支气管扩张剂、抗哮喘药、抗过敏药和抗胆碱药,其制备方法是:将 N-3-或 4-[4-吡啶基(CH2)n]苯基}-乙二醛酰胺肟与酸环化;将由此得到的产物与羰基反应试剂反应,制备 Q 为 0 以外的化合物;将 0 为 O 或 O 以外的化合物与强矿物酸的低级烷基、羟基低级烷基或二低级烷基氨基低级烷基酯或羧基低级烷氧基低级烷基卤化物反应,制备 R 为氢以外的化合物。