室温条件下无溶剂、无催化剂、绿色快速合成8-芳基-5,7,7-三氰基异喹啉衍生物

A Rapid and Green Synthesis of 8-Aryl-5,7,7-tricyanoisoquinoline Derivatives at Room Temperature under Solvent-Free and Catalyst-Free Conditions

芳醛、丙二腈和N-取代-4-哌啶酮在室温下,无溶剂、无催化剂反应,方便、快速地合成8-芳基-5,7,7-三氰基异喹啉衍生物.N-乙基-4-哌啶酮是首次应用于合成6-氨基-2-乙基-8-芳基-5,7,7(1H)-三氰基-2,3,8,8a-四氢异喹啉化合物.本方法具有反应条件温和、原料易得、操作简单、产率高、反应时间短,过程绿色等优点.产物的结构经过红外、核磁和高分辨质谱确定.本报道的方法是合成异喹啉类化合物的一条有效途径.

A facile and rapid synthesis of 8-aryl-5,7,7-tricyanoisoquinoline derivatives from the reaction of aromatic aldehydes, malononitrile, and N-substituted-4-piperidones at room temperature under solvent-free and catalyst-free conditions. The N-ethylpiperidin-4-one was first used for the synthesis of 6-amino-2-ethyl-8-aryl-2,3,8,Sa-tetrahydroisoquinoline-5,7,7（1^H）- tricarbonitrile derivatives. This method offers several advantages in terms of its mild conditions, available raw materials, simple operation, high yields, short reaction time and green process. The products were identified by IR, 1^H NMR and HRMS. The reported method is the efficient approach for the synthesis of isoquinoline derivatives.