Synthesis, biological activity, and absolute stereochemical assignment of NPS 1392: a potent and stereoselective NMDA receptor antagonist

Enantioselective Synthesis of β‐Methyl Amines via Iridium‐Catalyzed Asymmetric Hydrogenation of N‐Sulfonyl Allyl Amines

“…[1,2] Amines bearing a βmethyl stereogenic center are present in numerous bioactive compounds and pharmaceuticals. [3][4][5] Several examples of this type of drugs are shown in Figure 1. For example, Lorcaserin is a marketed anorectic for which a synthesis based on asymmetric hydrogenation have not been described to date.…”

“…[4] NPS-1392 is a potent stereoselective antagonist of the NMDA receptor. [5] The asymmetric hydrogenation is one of the most important catalytic reactions in the preparation of pharmaceuticals due to its atom economy, low environmental impact and operational simplicity. [6] Ru or Rh catalysts, which usually bear chiral phosphines, can induce high enantioselectivity on substrates functionalized with a coordinating group.…”