1446238-96-5Relevant articles and documents
Enantioselective synthesis of almorexant via iridium-catalysed intramolecular allylic amidation
Fa?anás-Mastral, Martín,Teichert, Johannes F.,Fernández-Salas, José Antonio,Heijnen, Dorus,Feringa, Ben L.
, p. 4521 - 4525 (2013/08/23)
An enantioselective synthesis of almorexant, a potent antagonist of human orexin receptors, is presented. The chiral tetrahydroisoquinoline core structure was prepared via iridium-catalysed asymmetric intramolecular allylic amidation. Further key catalytic steps of the synthesis include an oxidative Heck reaction at room temperature and a hydrazine-mediated organocatalysed reduction. The Royal Society of Chemistry 2013.