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    • 10. 发明授权
    • 3-keto-substituted-N-pyridylindoles
    • 3-酮取代的N-吡啶基吲哚
    • US4609733A
    • 1986-09-02
    • US686777
    • 1984-12-27
    • Stephen K. BoyerKarl O. GelotteJoseph Bach
    • Stephen K. BoyerKarl O. GelotteJoseph Bach
    • A61K31/44A61K31/4427A61P7/02A61P9/08A61P9/10A61P9/12C07D401/04
    • C07D401/04
    • Disclosed is a process for the preparation of a compound of the formula ##STR1## wherein Ar is 3- or 4-pyridyl or 3- or 4-pyridyl substituted by lower alkyl; R.sub.1 is hydrogen, halogen, trifluoromethyl, lower alkyl, hydroxy, acylated or etherified hydroxy, lower alkylthio; or two of R.sub.1 on adjacent carbon atoms represent alkylenedioxy; p is 1 or 2; R.sub.2 represents hydrogen or lower alkyl; E represents C.sub.1 -C.sub.11 alkylene, C.sub.1 -C.sub.6 alkylenephenylene, C.sub.1 -C.sub.6 alkylene-(thio or oxy)-lower alkylene, C.sub.1 -C.sub.6 alkylene-(thio or oxy)-phenylene, C.sub.1 -C.sub.6 alkylenephenylene-lower alkylene, phenylene-lower alkylene; or E represents a direct bond; and B represents carboxy, esterified carboxy or carbamoyl; which comprises deoxygenating the keto group in a compound of the formula ##STR2## wherein Ar, R.sub.1, R.sub.2, p, E and B have meaning as defined above.
    • 公开了制备式(I)的化合物的方法,其中Ar是3-或4-吡啶基或被低级烷基取代的3-或4-吡啶基; R1是氢,卤素,三氟甲基,低级烷基,羟基,酰化或醚化羟基,低级烷硫基; 或相邻碳原子上的R1中的两个表示亚烷基二氧基; p为1或2; R2代表氢或低级烷基; E表示C1-C11亚烷基,C1-C6亚烷基亚苯基,C1-C6亚烷基 - (硫代或氧基) - 低级亚烷基,C1-C6亚烷基 - (硫代或氧基) - 亚苯基,C1-C6亚烷基亚苯基 - 低级亚烷基,亚苯基低级 亚烷基 或E表示直接键; B代表羧基,酯化的羧基或氨基甲酰基; 其包括使式(Ⅳ)化合物中的酮基脱氧,其中Ar,R 1,R 2,p,E和B具有如上定义的含义。