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    • 3. 发明授权
    • Cyano containing indene derivatives
    • 含氰基的茚衍生物
    • US4873344A
    • 1989-10-10
    • US124820
    • 1987-11-24
    • Klaus P. BogesoMichael B. Sommer
    • Klaus P. BogesoMichael B. Sommer
    • C07C255/47C07C45/65C07C45/67C07C49/617C07C49/67C07C49/693C07C49/697C07C49/755C07C62/38C07C67/00C07C253/00C07C253/30C07C255/45C07C255/58C07C311/37C07C315/04C07C317/14C07C317/48C07C319/20C07C323/38C07C323/63C07D207/32C07D207/337C07D207/416C07D213/57C07D317/06C07D317/60C07D333/24
    • C07D207/337C07C255/00C07C45/676C07C49/697C07C62/38C07D213/57C07D317/60C07D333/24
    • The present invention relates to novel indene derivatives with the general formula I: ##STR1## wherein R.sup.1 is (a) a phenyl group optionally substituted with one or two groups selected from halogen, lower alkyl, lower alkoxy, lower alkylthio, lower alkylsulfonyl, dilower alkylamino, acylamino such as acetylamino, cyano, trifluoromethyl, trifluoromethoxy, pyrrole and dilower alkylpyrrole,(b) a polycyclic aromatic or heteroaromatic group, such as naphthalene or quinoline,(c) a heteroaromatic group such as thiophene, pyridine, and pyrrole, optionally substituted with one or more groups selected from halogen, lower alkyl, lower alkoxy, lower alkylthio, trifluoromethyl or trifluoromethoxy,R.sub.2 is selected from H, halogen, lower alkyl, benzyl, lower alkylthio, methoxy, lower alkylsulfonyl, dilower alkylsulfamoyl, acylamino such as acetylamino, benzylamino, dilower alkylamino, cyano, pyrrole, dilower alkylpyrrole, trifluoromethyl and trifluoromethoxy,R.sup.3 is CN, COOR.sup.4, --CON(R.sup.4).sub.2 or COR.sup.4, where R.sup.4 is a lower alkyl group, and "n" is an integer of from 1-3 inclusive.The indene derivatives of formula I are, when R.sup.1 is as defined under (a) above, valuable intermediates which are useful in the preparation of pharmacologically effective indane and indene derivatives known from e.g. U.S. Pat. Nos. 4,443,448 and 4,525,360.Moreover, the invention relates to a method for the preparation of the compounds of formula I and to a method for the preparation of compounds of the following formula IV: ##STR2## wherein R.sup.1, R.sup.2 and "n" are as defined above.
    • 本发明涉及具有通式I的新颖的茚衍生物:其中R 1是(a)任选被一个或两个选自卤素,低级烷基,低级烷氧基,低级烷硫基,低级烷基磺酰基, 二氯烷基氨基,酰氨基如乙酰氨基,氰基,三氟甲基,三氟甲氧基,吡咯和二烯烷基吡咯,(b)多环芳族或杂芳族基团如萘或喹啉,(c)杂芳基如噻吩,吡啶和吡咯, 任选被一个或多个选自卤素,低级烷基,低级烷氧基,低级烷硫基,三氟甲基或三氟甲氧基的基团取代,R 2选自H,卤素,低级烷基,苄基,低级烷硫基,甲氧基,低级烷基磺酰基,二低级烷基氨磺酰基, 作为乙酰氨基,苄氨基,二元烷基氨基,氰基,吡咯,二元烷基吡咯,三氟甲基和三氟甲氧基,R3是CN,COOR4,-CON(R4)2或COR4,其中 R4是低级烷基,“n”是1-3的整数。 当R1如上述(a)中所定义时,式I的茚衍生物是有用的中间体,它们可用于制备药物学有效的二氢化茚和茚衍生物,其从例如, 美国专利 第4,443,448号和第4,525,360号。 此外,本发明涉及制备式I化合物的方法和制备下式IV化合物的方法:其中R 1,R 2和“n”如上所定义。