Dipartimento di Chimica e Biologia "A. Zambelli", Università degli Studi di Salerno, Via Giovanni Paolo II, 84084 Fisciano, Italy.
Dipartimento di Scienze e Tecnologia, Università degli Studi del Sannio, Via De Sanctis, 82100 Benevento, Italy.
Molecules. 2022 Sep 1;27(17):5647. doi: 10.3390/molecules27175647.
Herein, we report the application of an efficient and practical KCO promoted cascade reaction of 2-acetylbenzonitrile in the synthesis of novel 3-methylated analogs of Pazinaclone and PD172938, belonging to isoindolinones heterocyclic class bearing a tetrasubstituted stereocenter. Organocatalytic asymmetric synthesis of the key intermediate and its transformation into highly enantioenriched 3-methylated analog of ()-PD172938 was also developed. These achievements can be of particular interest also for medicinal chemistry, since the methyl group is a very useful structural modification in the rational design of new and more effective bioactive compounds.
在此，我们报告了一种有效的、实用的 KCO 促进的 2-乙酰苯甲腈级联反应在新型 Pazinaclone 和 PD172938 的 3-甲基类似物合成中的应用，它们属于具有四取代立体中心的异吲哚啉酮杂环类。还开发了关键中间体的有机催化不对称合成及其转化为高度对映富集的（）-PD172938 的 3-甲基类似物。这些成就对于药物化学也特别有意义，因为甲基是合理设计新型、更有效的生物活性化合物的非常有用的结构修饰。
