发明授权
- 专利标题: Process for preparing pyridine-2-carboxamides
- 专利标题(中): 制备吡啶-2-甲酰胺的方法
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申请号: US304460申请日: 1994-09-12
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公开(公告)号: US5534635A公开(公告)日: 1996-07-09
- 发明人: Michelangelo Scalone , Peter Vogt
- 申请人: Michelangelo Scalone , Peter Vogt
- 申请人地址: NJ Nutley
- 专利权人: Hoffmann-La Roche Inc.
- 当前专利权人: Hoffmann-La Roche Inc.
- 当前专利权人地址: NJ Nutley
- 优先权: CHX736/89 19890228; CHX4323/89 19891204
- 主分类号: B01J31/24
- IPC分类号: B01J31/24 ; C07B61/00 ; C07D213/81 ; C07D213/56
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.
公开/授权文献
- US4407142A Heat recovery 公开/授权日:1983-10-04
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