发明授权
US06472532B1 Processes for the manufacturing of 3-hydroxy-n,1,6-trialkyl-4-OXO-1,4-dihydropyridine-2-carboxamide
失效
制备3-羟基-n，1,6-三烷基-4-氧代-1,4-二氢吡啶-2-甲酰胺的方法
- 专利标题： Processes for the manufacturing of 3-hydroxy-n,1,6-trialkyl-4-OXO-1,4-dihydropyridine-2-carboxamide
- 专利标题（中）： 制备3-羟基-n，1,6-三烷基-4-氧代-1,4-二氢吡啶-2-甲酰胺的方法
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申请号： US10100133申请日： 2002-03-19
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公开(公告)号： US06472532B1公开(公告)日： 2002-10-29
- 发明人: Tim F. Tam , Wanren Li
- 申请人： Tim F. Tam , Wanren Li
- 主分类号： C07D21186
- IPC分类号： C07D21186
摘要：
The present invention relates to a novel process for the preparation of 3-hydroxy-N,1,6-trialkyl-4-oxo-1,4-dihydropyridine-2-carboxamide of formula I: The method comprises of the TEMPO oxidation of a primary alcohol of 3-O-protected-2-hydroxymethyl-6-alkyl-4H-pyran-4-one of formula III to 3-O-protected-4-alkyl-4-oxo-4H-pyran-2-carboxylic acid of formula II. Reaction of compound of formula II with methylamine and 1,1-carbonyidiimidazole in an inert solvent affords 3-O-protected-N,1,6-trialkyl-4-oxo-1,4-dihydropyridine-2-carboxamide, which is deprotected to give of 3-hydroxy-N,1,6-trialkyl-4-oxo-1,4-dihydropyridine-2-carboxamide of formula I.
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