PROCEDE DE PREPARATION D'UN DERIVE D'ACIDE BENZOFURANE CARBOXYLIQUE OPTIQUEMENT PUR, ET SON UTILISATION POUR PREPARER L'EFAROXAN
    24.
    发明公开
    PROCEDE DE PREPARATION D'UN DERIVE D'ACIDE BENZOFURANE CARBOXYLIQUE OPTIQUEMENT PUR, ET SON UTILISATION POUR PREPARER L'EFAROXAN 失效
    方法用于制造光学纯BENZOFURANCARBONSÄUREDERIVATES及其用途用于生产依法克生

    公开(公告)号:EP0824531A1

    公开(公告)日:1998-02-25

    申请号:EP96919883.0

    申请日:1996-05-09

    IPC分类号: C07D307 C07D405

    CPC分类号: C07D405/04 C07D307/85

    摘要: A novel method for preparing an optically pure 2-ethyl-2,3-dihydro-benzofurancarboxylic acid derivative of general formula (II) is described, wherein R is a hydrogen atom, a halogen, a lower alkyl, lower alkoxy or hydroxy radical. The method comprises separating the racemic mixture by selective crystallisation with the suitable optically pure enantiomer of 2-phenylglycinol, in a suitable solvent, whereafter the optically pure, crystallised acid of formula (II) is isolated and recovered. The invention also provides the optically pure 2-ethyl-2,3-dihydro-benzofurancarboxylic acid derivative thus obtained and the use thereof for the preparation of an optically pure derivative of efaroxan.

    NOUVEAUX DERIVES AMIDES HETEROAROMATIQUES DE 3BETA-AMINO AZABICYCLOOCTANE, LEUR PROCEDE DE PREPARATION ET LEURS APPLICATIONS EN THERAPEUTIQUE
    27.
    发明公开
    NOUVEAUX DERIVES AMIDES HETEROAROMATIQUES DE 3BETA-AMINO AZABICYCLOOCTANE, LEUR PROCEDE DE PREPARATION ET LEURS APPLICATIONS EN THERAPEUTIQUE 有权
    它们的使用以及它们的治疗烷-3β-AMINOAZABICYCLOOCTANEN,PROCESS的NEW杂芳族酰胺衍生物

    公开(公告)号:EP1440075A1

    公开(公告)日:2004-07-28

    申请号:EP02785568.3

    申请日:2002-10-30

    CPC分类号: C07D491/04 C07D495/04

    摘要: The invention concerns compounds of general formula 1, wherein: A, B, D and E represent one or two nitrogen atoms, the others being carbon atoms; X represents a S or, a O, thereby forming a bicyclic fused heteroaromatic, such as thieno[2,3-b]pyridine, furo[2,3-b]pyridine, thieno[3,2-b]pyridine, furo[3,2-b]pyridine, thieno[2,3-b]pyrazine, furo[2,3-b]pyrazine, thieno[2,3-c]pyridine, furo[2,3-c]pyridine, thieno[3,2-c]pyridine and furo[3,2-c]pyridine; R1 represents a linear or branched C1-C6 alkoxy group, a linear or branched C1-C6 alkylthio group; R2 represents a linear, branched, cyclic C2-C8 group, a 2- or 3- thienylmethyl group, or a benzyl group optionally substituted by one or several halogens, F, Cl, Br, I, C1-C4 alkyl, C1-C4 alkoxy, CF3, CN, NO2, OH; and their pharmaceutically acceptable salts. Said compounds are anti-dopaminergic agents.