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 %.