Modular synthesis of chiral 1,2-dihydropyridines via Mannich/Wittig/cycloisomerization sequence that internally reuses waste

Abstract

1,2-Dihydropyridines are valuable precursors for the synthesis of biologically relevant piperidines and pyridines, but the methods for their synthesis are underdeveloped. Here, the authors report a modular organocatalytic Mannich/Wittig/cycloisomerization sequence to access chiral 1,2-dihydropyridines from N-Boc aldimines, aldehydes and phosphoranes, using a chiral amine catalyst.