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    Process for preparing pyridine-2-carboxamides
    10.
    发明授权
    Process for preparing pyridine-2-carboxamides 失效
    制备吡啶-2-甲酰胺的方法

    公开(公告)号：US5534635A

    公开(公告)日：1996-07-09

    申请号：US304460

    申请日：1994-09-12

    申请人： Michelangelo Scalone ,  Peter Vogt

    发明人： Michelangelo Scalone ,  Peter Vogt

    IPC分类号： B01J31/24 ,  C07B61/00 ,  C07D213/81 ,  C07D213/56

    CPC分类号： B01J31/2452 ,  B01J31/0237 ,  B01J31/1845 ,  B01J31/2295 ,  B01J31/24 ,  B01J31/2404 ,  B01J31/2409 ,  B01J31/2414 ,  C07D213/81 ,  B01J2231/34 ,  B01J2231/4205 ,  B01J2231/4266 ,  B01J2231/4283 ,  B01J2531/0205 ,  B01J2531/824 ,  B01J2531/842 ,  B01J31/0235

    摘要： It has been found that pyridine-2-carboxamides of the formula ##STR1## wherein R is amino or a residue convertible into amino, and pharmaceutically usable acid addition salts of that carboxamide in which R is amino can be prepared in a simple manner and in good yield by reacting 2,5-dichloropyridine in the presence of a palladium-phosphine catalyst with an alkyne of the formulaR.sup.1 --C.tbd.CH IIIwherein R.sup.1 is hydrogen, lower-alkyl, trimethylsilyl or the group --(R.sup.2)(R.sup.3)--COH and R.sup.2 and R.sup.3 each independently are hydrogen or lower-alkyl or together are cyclopentyl or cyclohexyl,oxidizing the resulting alkyne to give 5-chloropyridine-2-carboxylic acid and reacting this acid or a reactive functional derivative thereof with an amino compound of the formulaor with carbon monoxide and an amino compound of formula VI or with carbon monoxide and a lower alkanol which is optionally mixed with water and reacting the resulting acid or the resulting ester with an amino compound of formula VI. The compound of formula I in which R is amino is a known compound which is a reversible and highly active MAO-B inhibitor.

    摘要翻译： 已经发现，其中R是氨基或可转化成氨基的残基的式I的吡啶-2-甲酰胺和其中R是氨基的该甲酰胺的药学上可用的酸加成盐可以以简单的方式制备， 在钯 - 膦催化剂存在下与式R 1 -C 3的CH 2 CH 3其中R 1是氢，低级烷基，三甲基甲硅烷基或 - （R 2）（R 3）基团的反应，使2,5-二氯吡啶反应， -COH和R 2和R 3各自独立地为氢或低级烷基或一起为环戊基或环己基，氧化得到的炔烃，得到5-氯吡啶-2-羧酸，并使该酸或其反应性官能衍生物与 式或与一氧化碳和式VI的氨基化合物或一氧化碳和低级链烷醇反应，任选与水混合，并使所得酸或所得酯与式VI的氨基化合物反应。 其中R是氨基的式I化合物是已知的化合物，其是可逆的和高活性的MAO-B抑制剂。