1. A Nitrogen-Assisted One-Pot Heteroaryl Ketone Synthesis from Carboxylic Acids and Heteroaryl Halides
- Author
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Kazushi Hosoi, Yoichiro Ishimaru, Hirofumi Araki, Naotaka Sawada, Yoshimasa Omori, Tadashi Hukui, Erin O’Brien, Hideya Mizufune, Krystyna Demkiw, Eric L. Elliott, Frederick Hicks, Lei Zhu, Yasuhiro Sawai, Masahiro Mineno, Yoonjoo Fukuzumi, and Christopher L. Franklin
- Subjects
010405 organic chemistry ,Organic Chemistry ,Ketone synthesis ,chemistry.chemical_element ,Substrate (chemistry) ,Halide ,Ketone formation ,010402 general chemistry ,01 natural sciences ,Nitrogen ,0104 chemical sciences ,Catalysis ,chemistry.chemical_compound ,chemistry ,Functional group ,Organic chemistry ,Derivatization - Abstract
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.
- Published
- 2016