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Facile Access to 3-Unsubstituted Tetrahydroisoquinolonic Acids via the Castagnoli–Cushman Reaction
Synthesis ( IF 2.2 ) Pub Date : 2018-02-27 , DOI: 10.1055/s-0036-1591923
Natalia Guranova 1 , Dmitry Dar’in 1 , Mikhail Krasavin 1
Affiliation  

Abstract

Hitherto undescribed 3-unsubstituted tetrahydroisoquinolonic acids (isolated as their respective methyl esters) were accessed for the first time by the uncatalyzed, thermally promoted Castagnoli–Cushman reaction (CCR) of homophthalic anhydride (HPA) and a series of 1,3,5-triazinanes. The moderate yields observed in some cases are most likely associated with a persistent impurity also formed in these reactions. The new scaffold is expected to find novel medicinal utility (compared to the traditional CCR adducts) because it lacks a substituent at the 3-position.

Hitherto undescribed 3-unsubstituted tetrahydroisoquinolonic acids (isolated as their respective methyl esters) were accessed for the first time by the uncatalyzed, thermally promoted Castagnoli–Cushman reaction (CCR) of homophthalic anhydride (HPA) and a series of 1,3,5-triazinanes. The moderate yields observed in some cases are most likely associated with a persistent impurity also formed in these reactions. The new scaffold is expected to find novel medicinal utility (compared to the traditional CCR adducts) because it lacks a substituent at the 3-position.



中文翻译:

通过Castagnoli–Cushman反应轻松获得3-未取代的四氢异喹啉酸

摘要

迄今为止,未描述的3-未取代的四氢异喹啉酸(分别分离为各自的甲酯)是通过未催化的,热促进的高邻苯二甲酸酐(HPA)的Castagnoli-Cushman反应(CCR)和一系列1,3,5-而获得的。三嗪类。在某些情况下,观察到的中等产率很可能与在这些反应中也形成的持久性杂质有关。新的支架有望发现新的医学用途(与传统的CCR加合物相比),因为它在3位上没有取代基。

迄今为止,未描述的3-未取代的四氢异喹啉酸(分别分离为各自的甲酯)是通过未催化的,热促进的高邻苯二甲酸酐(HPA)的Castagnoli-Cushman反应(CCR)和一系列1,3,5-而获得的。三嗪类。在某些情况下,观察到的中等产率很可能与在这些反应中也形成的持久性杂质有关。新的支架有望发现新的医学用途(与传统的CCR加合物相比),因为它在3位上没有取代基。

更新日期:2018-02-27
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