4.8 Article

Base-Mediated [3+4]-Cycloaddition of Anthranils with Azaoxyallyl Cations: A New Approach to Multisubstituted Benzodiazepines

Journal

ORGANIC LETTERS
Volume 21, Issue 16, Pages 6245-6248

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.9b02118

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Funding

  1. Special Project of China [2018ZX097201003]
  2. National Science Foundation of China [81703332]

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A new [3 + 4] cycloaddition of azaoxyallyl cations and anthranils has been achieved for rapid access to multisubstituted benzodiazepine derivatives. A variety of anthranils and alpha-halo hydroxamates were both effective substrates with simple operations under transition-metal-free conditions. The intriguing features of this method include its mild nature of the reaction conditions, high efficiency, broad substrate scope, and wide functional group compatibility.

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