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Asymmetric Organocatalytic Biginelli Reactions:A New Approach To Quickly Access Optically Active 3,4-Dihydropyrimidin-2-(1H)-ones

机译:不对称有机催化大单反应:一种快速进入光学活性的3,4-二氢嘧啶-2-(1H) - 酮的新方法

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摘要

The Biginelli reaction,known for over 100 years,is an important multicomponent reaction for accessing dihydropyrimidinones(DHPMs).The individual enantiomers of DHPMs exhibit different or even opposite pharmaceutical activities,which require synthetic methods to easily access the optically pure DHPMs.In recent decades,many efforts have focused on developing procedures for the preparation of optically active Biginelli products.In this article,we will summarize the developments in the synthetic methods to access optically active DHPMs with an emphasis on the recent advances in the asymmetric catalytic Biginelli reactions,along with concepts to design the organocatalytic asymmetric variants.
机译:已知100多年的Biginelli反应是用于进入二氢嘧啶酮(DHPM)的重要多组分反应。DHPM的个体对映体表现出不同甚至相对的药物活性,这需要合成方法来容易进入光学纯粹的DHPMS。近几十年来 ,许多努力都集中在制定光学活性的Biginelli产品的程序方面。在本文中,我们将总结合成方法的开发,以强调不对称催化Biginelli反应的最近进步的重点 概念设计有机催化不对称变体。

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