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Communication | Special issue | Vol 79, No. 1, 2009, pp.319-324
Published online, 1st September, 2008
DOI: 10.3987/COM-08-S(D)6
Palladium-Catalyzed Heteroarylamination of Ethyl 2-Chloro-1-azaazulene-3-carboxylate and Annulation of Heteroarylamino-1-azaazurenes

Kazuya Koizumi, Kunitaka Shimabara, Aya Takemoto, Shinya Yamazaki, Noriko Yamauchi, Hiroyuki Fujii, Masaki Kurosawa, Takeo Konakahara, and Noritaka Abe*

*Applied Molecular Bioscience, Graduate School of Medicine, and Department of Biology and Chemistry, Faculty of Science, Yamaguchi University, Yoshida, Yamaguchi 753-8512, Japan


The palladium catalyzed heteroarylamination of ethyl 2-chloro-1-azaazulene-3-carboxylate was achieved using a catalyst based on Pd2(dba)3 / Xantphos system. Treatment of ethyl 2-(heteroarylamino)-1-aza-azulene-3-carboxylates with a PPA-POCl3 mixture gave corresponding annulation products. 2-(2-Benzothiazolylamino)-1-azaazulene (3h) showed anticancer activity against HeLa S3 cells (IC50: 6.5 μM).