Diversity-oriented synthesis of 1,3-benzodiazepines

作者：Wang, Gaigai; Liu, Chao; Li, Binbin; Wang, Yingchun; Van Hecke, Kristof; Van der Eycken, Erik V.; Pereshivko, Olga P.^*; Peshkov, Vsevolod A.^*

来源：Tetrahedron, 2017, 73(44): 6372-6380.

DOI：10.1016/j.tet.2017.09.034

• A(3)-coupling
• Propargylamines
• Isocyanates
• Reductive Heck reaction
• 1,3-Benzodiazepines
• Medium-rings

A concise assembly of the 1,3-benzodiazepine core from A(3')-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.

• 出版日期2017-11-2
• 单位苏州大学