GSK1360707F is a potent and selective triple reuptake inhibitor. It is chemically related to amitifadine and NS-2359 (GSK-372,475). Until recently, it was under development for the treatment of major depressive disorder; its development was put on hold for strategic reasons.
Synthesis
BOC Protecting group. Enolization and trapping with triflate group (cf Comins' reagent). Suzuki reaction Reduction (only 1 mol eq. LAH because N-BOC can be reduced to N-Me) Trifluoroacetic acid (TFA) removal of protecting group. Simmons–Smith reaction cyclopropanation. Williamson ether synthesis (c.f. NS patents & paxil).
Transporter occupancy GSK1360707F has recently (2013) been tested on baboons (Papio anubis) & humans for transporter occupancy using PET.
See also NS-2359
References