Diversity-oriented synthesis of 1,3-benzodiazepines
2017
Wang, Gaigai | Liu, Chao | Li, Binbin | Wang, Yingchun | Van Hecke, Kristof | Van der Eycken, Erik V. | Pereshivko, Olga P. | Peshkov, Vsevolod A.
A concise assembly of the 1,3-benzodiazepine core from A3-coupling-derived propargylamines and ortho-bromophenylisocyanates is described. The developed synthetic sequence involves the addition of propargylamine to isocyanate followed by palladium-catalyzed intramolecular alkyne hydroarylation that could be accomplished in a stepwise or one-pot manner.
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