Copper-Promoted Cyclization of α-Amino Nitrile-Tethered Enynes: Controllable Synthesis of 3-Azabicyclo[4.1.0]hepta-2,4-dienes and 4,5-Dihydro-3H-azepines

Org Lett. 2016 Aug 5;18(15):3854-7. doi: 10.1021/acs.orglett.6b01864. Epub 2016 Jul 27.

Abstract

The first example of Cu-promoted cyclization of α-amino nitrile-tethered enynes incorporating an electron-deficient alkene component is described. A wide range of functionalized 3-azabicyclo[4.1.0]hepta-2,4-dienes and 4,5-dihydro-3H-azepines were prepared efficiently in a controllable manner. Moreover, the diverse cascade process enables efficient incorporation of tertiary amine moieties under mild reaction conditions. A possible reaction pathway is proposed on the basis of a series of control experiments.

Publication types

  • Research Support, Non-U.S. Gov't