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Obituary
Yoshito Kishi (1937-2023)
Yoshito Kishi (1937-2023)
Professor. Yoshito Kishi,
a member of the Honorary Editorial Associates of HETEROCYCLES,
has passed away on January 9, 2023 at the age of 85.
I deeply express my regret over his death.
Kunio Ogasawara
Editor
January 13, 2023
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Communication | Special issue | Vol 79, No. 1, 2009, pp.319-324
Published online, 1st September, 2008■ Palladium-Catalyzed Heteroarylamination of Ethyl 2-Chloro-1-azaazulene-3-carboxylate and Annulation of Heteroarylamino-1-azaazurenes
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
Abstract
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).
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