Effective synthesis of enantiopure [1,2,3]triazolo[1,5-a]- and pyrazolo[1,5-a]pyrrolo[2,1-c][1,4]benzodiazepines by diastereoselective intramolecular azide and nitrilimine cycloadditions

摘要

The synthesis of new tetracyclic 1,4-benzodiazepinonic systems was performed in enantiopure form by totally diastereoselective intramolecular 1,3-dipolar cycloadditions. The absolute stereochemistry of the products was confirmed by X-ray crystallography and the enantiomeric purity was determined by using chiral HPLC.