GSK1360707F


GSK1360707F is a potent and selective triple reuptake inhibitor. It is chemically related to amitifadine and NS-2359. Until recently, it was under development for the treatment of major [depressive disorder]; its development was put on hold for strategic reasons.

Synthesis

  1. BOC Protecting group.
  2. Enolization and trapping with triflate group.
  3. Suzuki reaction
  4. Reduction
  5. Trifluoroacetic acid removal of protecting group.
  6. Simmons–Smith reaction cyclopropanation.
  7. Williamson [ether synthesis].

Transporter occupancy

GSK1360707F has recently been tested on baboons & humans for transporter occupancy using Positron [emission tomography|PET].