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1. 发明授权

US5977369A Process to prepare dihydropyridine and derivatives thereof 失效
标题翻译：二氢吡啶及其衍生物的制备方法
公开(公告)号：US5977369A
公开(公告)日：1999-11-02
申请号：US579758
申请日：1995-12-28
申请人： Ranjit Desai , Daniel Alfonso Aguilar , Mohammad Aslam , Nicholas Gallegos
发明人： Ranjit Desai , Daniel Alfonso Aguilar , Mohammad Aslam , Nicholas Gallegos
IPC分类号： C07D211/90 , C07D211/86
CPC分类号： C07D211/90
摘要： A novel process is disclosed for the preparation of dihydropyridine compounds and derivatives thereof, and more particularly felodipine. The process to prepare felodipine involves a two step procedure condensing 2,3-dichlorobenzaldehyde with methyl acetoacetate in the presence of a catalyst system. The resultant benzylidine intermediate is sequentially reacted with ethyl aminocrotonate to provide felodipine. The novelty of the present invention resides in part on (1) a new catalyst system not previously disclosed for the preparation of felodipine, (2) the absence of acid(s), (3) the control of reaction conditions to yield lower amounts of unreacted aldehyde compared to known reactions, (4) a simplified purification process, and (5) formation of negligible quantities of symmetrical diester byproducts.
摘要翻译：公开了制备二氢吡啶化合物及其衍生物，更特别是非洛地平的新方法。制备非洛地平的方法涉及在催化剂体系存在下将2,3-二氯苯甲醛与乙酰乙酸甲酯缩合的两步法。将所得的苄基中间体与氨基巴豆酸乙酯依次反应以提供非洛地平。本发明的新颖性部分在于（1）以前未公开制备非洛地平的新催化剂体系，（2）不存在酸，（3）控制反应条件以产生较低量的未反应的醛与已知的反应相比，（4）简化的纯化过程，和（5）形成可忽略量的对称的二酯副产物。

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