Ryoya Iioka, Kohei Yorozu, Yoko Sakai, Rika Kawai, Noriyuki Hatae, Katsuki Takashima, Genzoh Tanabe, Hiroaki Wasada, Mitsuhiro Yoshimatsu
European Journal of Organic Chemistry WILEY-V C H VERLAG GMBH 2021 (10) 1553 - 1558 1434-193X 2021/03
[Refereed] Lewis acid-catalyzed [6+1] annulation reactions of 2-cyano-1-propargyl- and 2-alkynyl-1-cyanomethyl-indoles with Reformatsky reagent are described. 8-Aryl, 8-alkyl-, 8-hetaryl-, 9-aryl, and 9-alkyl-azepino[1,2-a]indole amines were obtained through a 7-endo-mode cyclization of the beta-aminoacrylate intermediates. The antiproliferative activity of the azepino[1,2-a]indoles analogs against the HCT-116 cells were also examined.