Department of Chemistry, Fudan University, 220 Handan Road, Shanghai 200433, China.
Org Lett. 2011 Aug 19;13(16):4312-5. doi: 10.1021/ol201653j. Epub 2011 Jul 26.
A novel and efficient route for the synthesis of 2-amino-H-pyrazolo[5,1-a]isoquinolines via a three-component reaction of N'-(2-alkynylbenzylidene)hydrazide, alkyne, and sulfonyl azide is described. This transformation, co-catalyzed by silver triflate and copper(I) bromide under mild conditions, proceeds efficiently to generate the 2-amino-H-pyrazolo[5,1-a]isoquinolines in good to excellent yields.
通过 N'-(2-炔基苯亚甲基)腙、炔烃和磺酰叠氮的三组分反应,描述了一种合成 2-氨基-H-吡唑并[5,1-a]异喹啉的新颖高效途径。在温和条件下,三氟甲磺酸银和溴化亚铜共同催化下,该转化高效进行,以良好至优异的收率生成 2-氨基-H-吡唑并[5,1-a]异喹啉。