Journal
CHEMISTRY LETTERS
Volume 42, Issue 10, Pages 1260-1262Publisher
CHEMICAL SOC JAPAN
DOI: 10.1246/cl.130580
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Funding
- Grants-in-Aid for Scientific Research [25620119] Funding Source: KAKEN
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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.
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