Novel 4-membered azetidine nitrones💥 Ukaji & co-workers report a [2+1+1] approach: #diazomethane reacts with bulky nitrile oxides via double nucleophilic methylene incorporation ⚗️ Access to strained cyclic #nitrones opens new routes to biologically relevant #azetidines

👉 buff.ly/1vK9nXA

Structurally divergent reactivity of 2,2-disubstituted azetidines – mechanistic insights and stereochemical implications of amide coupling and ring expansion to 5,6-dihydro-4H-1,3-oxazines Azetidines have gained traction in drug discovery for their ability to introduce conformational constraint and modulate physiochemical properties. Strategies that enable their selective functionalizat...

🔔Open Access:
Structurally divergent reactivity of 2,2-disubstituted azetidines

by Alan C. Spivey et al.

🧪 Conditions tune azetidines to N-acylation or ring expansion → diverse heterocycles for drug discovery.

🔗 doi.org/10.1039/D5QO...
#Azetidines #Heterocycles #DrugDiscovery