- 著者
-
Kentaro Okuma
Yukiko Tanabe
Ryoichi Itoyama
Noriyoshi Nagahora
Kosei Shioji
- 出版者
- (社)日本化学会
- 雑誌
- Chemistry Letters (ISSN:03667022)
- 巻号頁・発行日
- vol.42, no.10, pp.1260-1262, 2013-10-05 (Released:2013-10-05)
- 参考文献数
- 22
- 被引用文献数
-
14
Novel one-pot synthesis of 2,3-benzodiazepines from aryne precursors was accomplished. Tofisopam, well-known anxiolytics, could be synthesized via C–C bond insertion of 4,5-dimethoxybenzyne with 2-ethyl-1-(3,4-dimethoxyphenyl)butane-1,3-dione, followed by the reaction with hydrazine hydrate in a one-pot operation. This protocol is applicable to the synthesis of other biologically active 2,3-benzodiazepines, such as Girisopam and Nerisopam.