发明名称 Process for production of piperidine derivatives and their use in the treatment of allergic reactions
摘要 Disclosed is a process for the preparation of piperidine derivative compounds of formula (I) and (II) wherein n is 0 or 1 R1 is hydrogen or hydroxy R2 is hydrogen, or when n is O, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen R3 is -COOH or -COOR4 R4 is an alkyl or aryl moiety A, B and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy and other substituents. The process comprises providing a regioisomer of formula (III), wherein Z is -CG1G2G3 (IV) or (V) m is an integer from 1 to 6 Q and Y are the same or different and are selected from the group consisting of O, S and NR5, G1, G2 and G3 are the same or different and are selected from the group consisting of OR8, SR8 and NR8R9 R6 and R7 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, an aryl moiety, OR8, SR8 and NR8R9 R5, R8 and R9 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety and converting the regioisomer to the piperidine derivative compound with a piperidine compound. Also disclosed is the use of piperidine derivatives of formula (I), such as á,á-disubstituted-methylbenzene for treating allergic reactions.
申请公布号 NZ326085(A) 申请公布日期 2001.04.27
申请号 NZ19960326085 申请日期 1996.12.19
申请人 ALBANY MOLECULAR RESEARCH, INC 发明人 D'AMBRA, THOMAS E;PILLING, GARRY M
分类号 C07D211/22;A61K31/00;A61K31/42;A61K31/421;A61K31/445;A61P37/00;A61P37/08;C07D211/14;C07D211/34;C07D211/44;C07D211/46;C07D263/10;(IPC1-7):A61K31/445 主分类号 C07D211/22
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