A Nitrogen-Assisted One-Pot Heteroaryl Ketone Synthesis from Carboxylic Acids and Heteroaryl Halides
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- 作者：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
- 刊名：Journal of Organic Chemistry
- 出版年：2016
- 出版时间：April 15, 2016
- 年：2016
- 卷：81
- 期：8
- 页码：3447-3456
- 全文大小：418K
- 年卷期：0
- ISSN：1520-6904
文摘
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.