PROCESS FOR PREPARING ARYLPIPERIDINE CARBINOL INTERMEDIATES AND DERIVATIVES
    6.
    发明公开
    PROCESS FOR PREPARING ARYLPIPERIDINE CARBINOL INTERMEDIATES AND DERIVATIVES 审中-公开
    用于生产ARYLPIPERIDINCARBINOL中间体及其衍生物

    公开(公告)号:EP1140832A4

    公开(公告)日:2004-11-03

    申请号:EP99966475

    申请日:1999-12-17

    摘要: A process for the synthesis of arylpiperidine carbinol intermediates and derivatives is disclosed. A preferred process embodiment provides the synthesis of intermediate compounds of structural formula (I) and structural formula (II), where X is halogen, C1-C10 alkyl, C1-C10 alkoxy, C1-C10 haloalkyl, hydroxy, or hydrogen; and R2 and R3 each is C1-C4 alkyl and R2 and R3 are the same. The compound of structural formula (I) is made by condensing a corresponding cinnamonitrile with a corresponding diester malonate. The compound of structural formula (II) in the (±)-trans configuration is obtained by hydrogenating the compound of structural formula (I). The compounds of structural formula (I) and structural formula (II) are useful chemical intermediates for synthesizing 4-arylpiperidine-3-carbinols and their derivatives in (-)-trans configuration.