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A Nitrogen-Assisted One-Pot Heteroaryl Ketone Synthesis from Carboxylic Acids and Heteroaryl Halides

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journal contribution
posted on 18.03.2016, 00:00 by Krystyna Demkiw, Hirofumi Araki, Eric L. Elliott, Christopher L. Franklin, Yoonjoo Fukuzumi, Frederick Hicks, Kazushi Hosoi, Tadashi Hukui, Yoichiro Ishimaru, Erin O’Brien, Yoshimasa Omori, Masahiro Mineno, Hideya Mizufune, Naotaka Sawada, Yasuhiro Sawai, Lei Zhu
A practical and highly effective one-pot synthesis of versatile heteroaryl ketones directly from carboxylic acids and heteroaryl halides under mild conditions is reported. This method does not require derivatization of carboxylic acids (preparation of acid chlorides, Weinreb amides, etc.) or the use of any additives/catalysts. A wide substrate scope of carboxylic acids with high functional group tolerance has also been demonstrated. The results reveal that the presence of an α-nitrogen on the halide substrate greatly improves the desired ketone formation.