We report an unexpected route for synthesizing pyrrole-fused dibenzoxazepines/thiazepines with high chemoselectivity via a pseudo-Joullié–Ugi reaction from cyclic imines with isocyanides and acetylenedicarboxylates under catalyst-free conditions.
An efficient visible-light-induced Staudinger [2 + 2] annulation reaction under catalyst-free conditions has been established, and tetracyclic dibenzo[b,f][1,4]oxazepine/thiazepine-fused β-lactams were synthesized with a broad substrate scope and high efficiency (37 examples, up to >99% yield).
SCD1 inhibitors block the conversion of saturated to monounsaturated fatty acids, reducing lipid accumulation, desaturation index, fat mass, and lipotoxicity. They are promising for treating various metabolic disorders.
Highly efficient asymmetric hydrogenation of dibenzo-fused azepines derivatives with chiral cationic Ru diamine catalysts has been developed, giving diverse chiral seven-membered N-heterocycles with excellent results (up to 99% yield and 99% ee).
Here, we describe the one-pot assembly of imidazo[1,2-a]pyridine and quinoxaline heterocyclic cores by the electrophilic tandem cyclization between 3,5-diaryl substituted 5-hydroxy-3-pyrrolin-2-ones and the corresponding nitrogen bis-nucleophiles.