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：

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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。