Aminotetralone derivatives and preparation process thereof
    67.
    发明授权
    Aminotetralone derivatives and preparation process thereof 失效
    氨基四氢萘酮衍生物及其制备方法

    公开(公告)号:US5849945A

    公开(公告)日:1998-12-15

    申请号:US894230

    申请日:1997-08-21

    摘要: The present invention pertains to a process for the preparation of Compound (4) through the below-described reaction route: ##STR1## wherein R.sup.1 and R.sup.2 each represents H, halogen, OH or C.sub.1-6 alkyl group; X and Y each represents a protected amino group and n stands for 0 to 4. According to the above process, an aminotetralone derivative which is an intermediate useful for an industrial preparation of a camptothecin derivative can be obtained in a convenient manner and in a high yield.

    摘要翻译: PCT No.PCT / JP96 / 00390 Sec。 371日期1997年8月21日 102(e)日期1997年8月21日PCT 1996年2月21日PCT PCT。 WO96 / 26181 PCT出版物 日期:1996年8月29日本发明涉及通过下述反应路线制备化合物(4)的方法:其中R1和R2各自表示H, 卤素,OH或C 1-6烷基; X和Y各自表示保护的氨基,n表示0至4.根据上述方法,可以以方便的方式获得作为用于喜树碱衍生物的工业制备的中间体的氨基四氢萘酮衍生物 产量。

    Substituted N-arylmethylamino derivatives of cyclobutene-3,4-diones
    68.
    发明授权
    Substituted N-arylmethylamino derivatives of cyclobutene-3,4-diones 失效
    取代的环丁烯-3,4-二酮的N-芳基甲基氨基衍生物

    公开(公告)号:US5763474A

    公开(公告)日:1998-06-09

    申请号:US889164

    申请日:1997-07-07

    摘要: The compounds of the formula: ##STR1## wherein R.sub.1 is straight chain alkyl, branched chain alkyl cycloalkyl, hydroxyalkyl, fluoroalkyl or polyfluoroalkyl; R.sub.2 and R.sub.3 are, independently, hydrogen or an acyl substituent selected from the group consisting of formyl, alkanoyl, alkenoyl, alkoxycarbonyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; A is a substituted phenyl group of the following formula: ##STR2## wherein R.sub.4 and R.sub.5 are, independently, cyano, nitro, amino, alkyl, perfluoroalkyl, fluoroalkyl, alkoxy, perfluoroalkoxy, fluoroalkoxy, amino, alkylamino, dialkylamino, sulfamyl, alkylsulfonamido, arylsulfonamido, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, alkylcarboxamido, arylcarboxamido, alkylsulfonyl, perfluoroalkylsulfonyl, arylsulfonyl, chloro, bromo, fluoro, iodo, 1-imidazolyl, carboxyl or hydrogen, with the proviso that R.sub.4 and R.sub.5 cannot both be hydrogen; or a pharmaceutically acceptable salt thereof, relaxes smooth muscles.

    摘要翻译: 下式的化合物:其中R 1是直链烷基,支链烷基环烷基,羟基烷基,氟烷基或多氟烷基; R2和R3独立地为氢或选自甲酰基,烷酰基,烯酰基,烷氧基羰基,烷基磺酰基,芳酰基,芳基烯酰基,芳基磺酰基,芳基烷酰基或芳基烷基磺酰基的酰基取代基。 A是下式的取代苯基:其中R 4和R 5独立地是氰基,硝基,氨基,烷基,全氟烷基,氟烷基,烷氧基,全氟烷氧基,氟烷氧基,氨基,烷基氨基,二烷基氨基,氨基磺酰基,烷基亚磺酰氨基, 芳基亚磺酰氨基,氨基甲酰基,烷基氨基甲酰基,二烷基氨基甲酰基,烷基酰胺基,芳基羧酰氨基,烷基磺酰基,全氟烷基磺酰基,芳基磺酰基,氯,溴,氟,碘,1-咪唑基,羧基或氢,条件是R4和R5不能都是氢; 或其药学上可接受的盐,使平滑肌松弛。