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    PROCESS FOR PREPARING 1,3-DIHYDROSPIRO (ISOBENZOFURAN-1,4-PIPERIDINE)S
    2.
    发明授权
    PROCESS FOR PREPARING 1,3-DIHYDROSPIRO (ISOBENZOFURAN-1,4-PIPERIDINE)S 失效

    公开(公告)号：KR810000892B1

    公开(公告)日：1981-08-17

    申请号：KR790004722

    申请日：1979-12-31

    Applicant: HOECHST AG

    Inventor： BAUER V ,  KLIOZE S

    IPC: C07D491/107

    Abstract: The title compds. (I; R = C1-4 alkyl or C7-9 phenalkyl; R1 = H, C1-3 alkoxy or trifluoromethyl; R2 = H, C1-3 alkoxy, Br, F or Cl) useful as analgesics, anticonvulsants, and antidepressants were manufd. by oxidation of piperidine(II) with org. or inorg. peroxide in the presence of org. solvent. Thus, 1-nitroso-1,3-dihydro-3-phenylspiro(isobenzofuran-1,4'-piperidine) was mixed with glacial acetic acid and extracted to give 1'-amino-1,3-dihydro-3-phenylspiro(isobenzofuran-1,4'-piperidine), which was reacted with sodium cyanoborohydride to give 1'-(isopropylamino)1,3'-dihydro-3-phenylspiro(isobenzofuran-1,4'-piperidine.

    METHODS FOR PREPARING 1,3 DIHYDRO SPIRO(ISOBENAOFURAN-1,4'-PIPERIDINES)
    3.
    发明授权
    METHODS FOR PREPARING 1,3 DIHYDRO SPIRO(ISOBENAOFURAN-1,4'-PIPERIDINES) 失效

    公开(公告)号：KR810000335B1

    公开(公告)日：1981-04-20

    申请号：KR750002152

    申请日：1975-10-02

    Applicant: HOECHST AG

    Inventor： KLIOZE S ,  BAUER V

    IPC: A61K31/445 ,  C07D491/10

    Abstract: Analgesic title compds. (I; X = nitroso, amino, C1-5alkyl amino, benzoyloxy, OH; R1 = H, C1-3 alkoxy, CF3; R2 = H, C1-3 alkoxy, Br, F, Cl) were prepd. by several method. Thus, II was converted to nitroso compd. at 0-5≦̸C, reduced to corresponding amino compd. and alkylated to corresponding alkylamino compd., or II was reacted with benzoylperoxide at 0-80≦̸C, 12 hr to give benzoyloxy compd. (III) and benzoyloxy group of III was eleminated to give corresponding hydroxy compd.

    PROCESS FOR PREPARING SUBSTITUTED 1,3-DIHYDROSPIRO(ISOBENZOFURAN)S
    4.
    发明授权
    PROCESS FOR PREPARING SUBSTITUTED 1,3-DIHYDROSPIRO(ISOBENZOFURAN)S 失效

    公开(公告)号：KR810000027B1

    公开(公告)日：1981-02-02

    申请号：KR750000027

    申请日：1975-01-09

    Applicant: HOECHST AG

    Inventor： BAUER V ,  KOSLEY R

    IPC: A61K31/34 ,  C07D307/87

    Abstract: Title compds. (I; R= H, C1-6 alkyl, C1-6 alkoxy, CF3, halogen, OH, methylenedioxy; R1 = H, C1-6 alkyl, C4-8 cycloalkyl, C3-6 alkenyl, phenylalkyl, etc.; R2 = C1-6 alkyl, phenyl; Y = H, C1-6 alkyl, C1-6 alkoxy, hydroxy phenyl; m or n = 1, 2, 3) and their acid addn. salts, with antidepressant, tranquilizing and analgesic effect, are prepd. by treating compd. (II) with organic metal reagent. In case of Y = OH, O-hydroxy alkyl phenyl-cycloazalkanol compd.(III) is obtained by reduction, which is cyclized with acid to give 1,3-dihydro spiro(isobenzofuran-cycloazalkane).

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