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 %.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.