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    6.
    发明专利
    未知

    公开(公告)号：ES2098357T3

    公开(公告)日：1997-05-01

    申请号：ES91911488

    申请日：1991-06-05

    Applicant: TORAY INDUSTRIES

    Inventor： NAGASE HIROSHI ,  MIZUSUNA AKIRA ,  ONODA YOSHIHIRO ,  KAWAI KOJI ,  MATSUMOTO SHU ,  ENDO TAKASHI

    IPC: C07D217/06 ,  C07D217/24 ,  C07D471/04 ,  C07D491/056 ,  A61K31/475

    Abstract: An isoquinoline derivative represented by the general formula (101): wherein R101 is a hydrogen atom or a C1-5 alkyl, C4-7 cycloalkylalkyl, C6-8 cycloalkenylalkyl, C7-14 aralkyl, C4-5 transalkenyl, allyl, furanyl-2-ylalkyl, thienyl-2-ylalkyl or R107OCO group (wherein R107 is a 2,2,2-trichloroethyl or benzyl group) or is a R108CO group (wherein R108 is a C1-5 alkyl, C3-6 cycloalkyl, C5-7 cycloalkenyl, phenyl, C7-13 aralkyl, C4-5 trans-alkenyl, vinyl, 2-furanyl or 2-thienyl group), R102, R103, R104 and R105 are each independently a hydrogen atom or a hydroxy, alkanoyloxy having up to 5 carbon atoms or C1-5 alkoxy group or wherein R102 and R103 jointly or R104 and R105 jointly may form oxo or R103 and R104 jointly may form a 1,3-dioxolan ring, R106 is a hydrogen atom or a hydroxy, C1-5 alkoxy or alkanoyloxy group having up to 5 carbon atoms and wherein the general formula (101) embraces a (+) form, a (-) form, and a (+/-) form, or a pharmacologically acceptable salt thereof; is prepared by oxidizing the carbamate form of an enamine represented by the general formula (103): wherein R102, R103, R104, R105, R106 and R107 are as defined above, thereby forming an oxide represented by the general formula (101a): wherein R102, R103, R104, R105, R106 and R107 are as defined above, and wherein the formula (101a) embraces a (+) form, a (-) form, and a (+/-) form; and optionally converting the group to any of the other values of the group R101. The compounds are intermediates for the production of pharmaceutically useful indole derivatives.

    9.
    发明专利
    未知

    公开(公告)号：FI920480A0

    公开(公告)日：1992-02-04

    申请号：FI920480

    申请日：1992-02-04

    Applicant: TORAY INDUSTRIES

    Inventor： NAGASE HIROSHI ,  MIZUSUNA AKIRA ,  ONODA YOSHIHIRO ,  KAWAI KOJI ,  MATSUMOTO SHU ,  ENDO TAKASHI

    IPC: C07D217/06 ,  C07D217/24 ,  C07D471/04 ,  C07D491/056 ,  C07D

    Abstract: An isoquinoline derivative represented by the general formula (101): wherein R101 is a hydrogen atom or a C1-5 alkyl, C4-7 cycloalkylalkyl, C6-8 cycloalkenylalkyl, C7-14 aralkyl, C4-5 transalkenyl, allyl, furanyl-2-ylalkyl, thienyl-2-ylalkyl or R107OCO group (wherein R107 is a 2,2,2-trichloroethyl or benzyl group) or is a R108CO group (wherein R108 is a C1-5 alkyl, C3-6 cycloalkyl, C5-7 cycloalkenyl, phenyl, C7-13 aralkyl, C4-5 trans-alkenyl, vinyl, 2-furanyl or 2-thienyl group), R102, R103, R104 and R105 are each independently a hydrogen atom or a hydroxy, alkanoyloxy having up to 5 carbon atoms or C1-5 alkoxy group or wherein R102 and R103 jointly or R104 and R105 jointly may form oxo or R103 and R104 jointly may form a 1,3-dioxolan ring, R106 is a hydrogen atom or a hydroxy, C1-5 alkoxy or alkanoyloxy group having up to 5 carbon atoms and wherein the general formula (101) embraces a (+) form, a (-) form, and a (+/-) form, or a pharmacologically acceptable salt thereof; is prepared by oxidizing the carbamate form of an enamine represented by the general formula (103): wherein R102, R103, R104, R105, R106 and R107 are as defined above, thereby forming an oxide represented by the general formula (101a): wherein R102, R103, R104, R105, R106 and R107 are as defined above, and wherein the formula (101a) embraces a (+) form, a (-) form, and a (+/-) form; and optionally converting the group to any of the other values of the group R101. The compounds are intermediates for the production of pharmaceutically useful indole derivatives.

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