单取代1,3-[2H,4H]-异喹啉二酮的合成

四氢异喹啉类生物碱在自然界分布广泛且活性多样,使得这一结构成为有机合成的热点,然而在众多的有机合成方法学中,绝大多数报道都是围绕着四氢异喹啉C-1位的官能团化,对C-4位活化的方法较少,本文从1,3-2H,4H]-异喹啉二酮出发经过两步反应即可得到4-取代的1,3-2H,4H]-异喹啉二酮,并以1HNMR,13CNMR和HRMS确定其化学结构。产物1,3-2H,4H]-异喹啉二酮可以根据文献报道方法得到4-取代四氢异喹啉化合物,为4-取代的四氢异喹啉类化合物的合成提供了一条便捷的路径。

Synthesis of 4-Substituted 1,3-[2H,4H]-Isoquinolinedione

Tetrahydroisoquinoline alkaloids are widely distributed in nature and bear diverse activity, the structure has become a hot spot for organic synthesis. However, most of the methods reported so far focus on the C-1 functionalization of tetrahydroisoquinoline, while the C-4 activation method is rare. This article use the 1,3-2H,4H]-isoquinolinedione as starting material and C-4 functionalized tetrahydroisoquinoline skeleton could be obtained in two steps, and the chemical structures are determined by 1HNMR, 13CNMR and HRMS. The product 1,3-2H, 4H]- isoquinolinedione can be transformed to tetrahydroisoquinoline compound using reported method, which provides a convenient route for the synthesis of tetrahydroisoquinoline compounds.