1312550-16-5Relevant articles and documents
Multi-substituted 8-aminoimidazo[1,2-a]pyrazines by Groebke-Blackburn-Bienaym reaction and their Hsp90 inhibitory activity
Ren, Jing,Yang, Min,Liu, Hongchun,Cao, Danyan,Chen, Danqi,Li, Jian,Tang, Le,He, Jianhua,Chen, Yue-Lei,Geng, Meiyu,Xiong, Bing,Shen, Jingkang
supporting information, p. 1531 - 1535 (2015/02/05)
Using a 2,3-diamino pyrazine substrate and yttrium triflate catalyst, various 2-alkyl and aryl substituted 3,8-diaminoimidazo[1,2-a]pyrazines were efficiently prepared through Groebke-Blackburn-Bienaym MCR. In particular, a novel 2-piperonyl 3,8-diaminoimidazo[1,2-a]pyrazine structure was prepared exclusively with this new method and was found to have moderate Hsp90 inhibitory activity. A crystalline complex with N-terminus ATP domain of Hsp90 and one of the new Hsp90 inhibitors was also obtained to elucidate the origin of activity of 2-piperonyl 3,8-diaminoimidazo[1,2-a]pyrazines.