一种合成N-芳基-3,4-二取代异喹啉酮类化合物的方法

A method for the synthesis of N-aryl-3,4-two substituted isoquinoline derivatives

N-芳基-3,4-二取代异喹啉酮类化合物是一类具有广泛生物活性和独特药理活性的杂环化合物,对该类化合物的合成研究一直是有机化学和药物化学领域的研究热点。以邻炔苯甲酰胺化合物为反应底物,在NaH作用下,以碳负离子作为亲核基团进攻炔基进行关环反应得到异喹啉酮类化合物,产物结构经核磁共振和质谱分析确证。该方法原料易得、反应条件温和、收率中等、易于引入各种取代基团,为异喹啉酮类化合物的结构修饰和衍生化发展提供了一种十分有效的方法。

N-aryl-3,4-disubstituted isoquinolinone are important heterocyclic compounds with a wide spectrum of biological activities and unique pharmacological activity.The synthesis of these compounds has been a research hotspot in organic chemistry and medicinal chemistry.In this study,based on the reaction of o-alkynylbenzamide with NaH,the isoquinoline compounds were obtained by cyclization reaction that used carbon negative ions as nucleophilic groups to attack alkynes.NMR and MS analysis have been performed to confirm the products.The synthetic method reported here has many advantages such as facilely accessible starting materials,mild reaction conditions,moderate yield and convenience to introduce various substituent groups,providing a highly effective way for structural modification and derivatization of isoquinoline compounds.