Zusammenfassung
Thefirst enantioselective synthesis of (S)-meptazi-nol in 14 steps from commercially available ethyl 4-oxo-3,4-dihydropyridine-1(2H)-carboxylate, being widely used in racemicform for pain treatment, and, en route, the formal synthesis of twoanti-Alzheimer's agents are reported. A novel ring expansion of 2-azabicyclo[4.1.0]heptanes, readily available via the stereoselectivecyclopropanation of ...
Zusammenfassung
Thefirst enantioselective synthesis of (S)-meptazi-nol in 14 steps from commercially available ethyl 4-oxo-3,4-dihydropyridine-1(2H)-carboxylate, being widely used in racemicform for pain treatment, and, en route, the formal synthesis of twoanti-Alzheimer's agents are reported. A novel ring expansion of 2-azabicyclo[4.1.0]heptanes, readily available via the stereoselectivecyclopropanation of 1,2,3,4-tetrahydropyridine-4-ols, provides aneffective entry to 3,3-disubstituted azepanes that represent the core for a variety of approved drugs.
Altmetric