Synthesis of New Chiral Triazoles Linked 1,5‐Benzodiazepine Conjugates via Copper‐Catalyzed 1,3‐Dipolar Cycloaddition Reaction

Abstract

A simple synthesis of 1,4‐disubstituted 1,2,3‐triazoles linked‐1,5‐benzodiazepinones was performed via a Cu(I)‐catalyzed 1,3‐dipolar alkyne‐azide coupling reaction (CuAAC). A new chiral 1,5‐benzodiazepine conjugates moiety containing alkyne spacers is designed and used as dipoles to give the access to the target cycloadducts with high yields. Both chiral center and freeze conformations allow to reach important diastereoselectivity from 70 up to 100 %.

A combined crystallographic and theoretical investigation of noncovalent interactions in 1,3,4-oxadiazole-2-thione-N-Mannich derivatives: in vitro bioactivity and molecular docking

“…53 Several nonclassical noncovalent interactions observed in molecular solids were described in the literature to highlight their cooperativity with conventional noncovalent interactions and the role of individual interaction in supramolecular assemblies. 54…”