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

    PROCESS FOR PREPARING 1,3-DIHYDRO-1'-DIMETHYL PHOSPHINYLALKYL-O-PHENYLSPIRO(ISOBENZO FURAN)S
    3.
    发明授权
    PROCESS FOR PREPARING 1,3-DIHYDRO-1'-DIMETHYL PHOSPHINYLALKYL-O-PHENYLSPIRO(ISOBENZO FURAN)S 失效

    公开(公告)号：KR800001555B1

    公开(公告)日：1980-12-27

    申请号：KR760001807

    申请日：1976-07-26

    Applicant: HOECHST AG

    Inventor： KLIOZE S

    IPC: C07D405/04

    Abstract: Title compds. (I; R, R1 = H, lower alkyl, lower alkoxy, halogen or hydroxy group; m, m; = 1,2; n, n' = 1,2,3; p = 1-4),useful for treatment of melancholia, were prepd. by reaction of 1,3-dihydro-3-phenylspiro(isobenzofuran-cycloazalkane)(II; R;, R1 = H, lower alkyl, lower alkoxy, halogen) with compd.(III; X = Cl, Br; q = 0, 1, 2, 3) in the presence of org. solvent and acid eliminating agent. Thus, K2CO3 3.0g and chloromethyldimethylphosphineoxide 1.39g were added in the 1,3-dihydro-3-phenylspiro(isobenzofuran-1,4;-piperidine) 2.65g in dimethylformamide 40ml soln. and heated at 100≦̸C for 20hr to give compd.(I).

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