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连续流动逆狄尔斯-阿尔德反应:一种制备嘧啶酮衍生物的有效方法。

Continuous-flow retro-Diels-Alder reaction: an efficient method for the preparation of pyrimidinone derivatives.

作者信息

Nekkaa Imane, Palkó Márta, Mándity István M, Fülöp Ferenc

机构信息

Institute of Pharmaceutical Chemistry, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary.

MTA-SZTE Stereochemistry Research Group, Hungarian Academy of Sciences, Eötvös u. 6, H-6720 Szeged, Hungary.

出版信息

Beilstein J Org Chem. 2018 Feb 1;14:318-324. doi: 10.3762/bjoc.14.20. eCollection 2018.

Abstract

The syntheses of various pyrimidinones as potentially bioactive products by means of the highly controlled continuous-flow retro-Diels-Alder reaction of condensed pyrimidinone derivatives are presented. Noteworthy, the use of this approach allowed us to rapidly screen a selection of conditions and quickly confirm the viability of preparing the desired pyrimidinones in short reaction times. Yields typically higher than those published earlier using conventional batch or microwave processes were achieved.

摘要

本文介绍了通过稠合嘧啶酮衍生物的高度可控连续流逆狄尔斯-阿尔德反应合成各种具有潜在生物活性的嘧啶酮。值得注意的是,使用这种方法使我们能够快速筛选一系列条件,并迅速确认在短反应时间内制备所需嘧啶酮的可行性。获得的产率通常高于早期使用传统间歇或微波方法所报道的产率。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2a53/5815275/4975008079ef/Beilstein_J_Org_Chem-14-318-g003.jpg

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