Method for the synthesis of pharmacologically active compounds and
intermediates for such synthesis
    4.
    发明授权
    Method for the synthesis of pharmacologically active compounds and intermediates for such synthesis 失效
    用于合成药理学活性化合物的方法和用于这种合成的中间体

    公开(公告)号:US4777293A

    公开(公告)日:1988-10-11

    申请号:US753682

    申请日:1985-07-10

    申请人: Bo R. Lamm

    发明人: Bo R. Lamm

    摘要: A process for the preparation of an aryloxypropanolamine of the formulaAr--OCH.sub.2 CH(OH)CH.sub.2 NH--R Iwherein Ar is a carbocyclic or heterocyclic aromatic group and R is an alkyl or substituted alkyl group having 1 to 6 carbon atoms, characterized in subjecting a compound of the formula ##STR1## to oxidative cleavage to a dialdehyde of the formula ##STR2## which is then made subject to reduction, amination, acetal hydrolysis, and, where required, removal of a nitrogen protective group, to the formation of a compound of formula I, or an acid addition salt thereof, a compound of formula II and the preparation thereof from mannitol.

    摘要翻译: 一种制备式Ar-OCH 2 CH(OH)CH 2 NH-RI的芳氧基丙醇胺的方法,其中Ar是碳环或杂环芳族基团,R是具有1至6个碳原子的烷基或取代的烷基,其特征在于使化合物 式II的氧化裂解制成式“IMAGE”III的二醛,然后将其还原,胺化,缩醛水解,并且在需要时除去氮保护基团以形成 式I化合物或其酸加成盐,式II化合物及其从甘露醇制备。