Get access

Synthesis of Azepine Derivatives by Rhodium-Catalyzed Tandem 2,3-Rearrangement/Heterocyclization


  • This work was supported by a Grant-in-Aid for Scientific Research on Innovative Areas “Molecular Activation Directed toward Straightforward Synthesis” from the Ministry of Education, Culture, Sports, Science and Technology (Japan).


original image

Easy to N-cycle: The efficient synthesis of azepine derivatives was achieved by Rh-catalyzed tandem 2,3-rearrangement involving the heterocyclization of N-allenylnitrone intermediates (see scheme; cod=1,5-cyclooctadiene, tppms=sodium diphenylphosphinobenzene-3-sulfonate).