A PASE-based approach towards 12-(1H-1,2,3-triazol-1-yl)indolo[2,1-a]isoquinolines via the reaction of 3-(isoquinolin-1-yl)-1,2,4-triazines with benzyne

摘要

12-(1H-1,2,3-Triazol-1-ypindolo[2,1-a]isoquinolines are prepared in 51-56% yields using a PASE (pot, atom, step, economic)-based approach, namely, by the reaction between available 5-R-6-Ar-3-(isoquinolin-l-yl)-1,2,4-triazines and in situ generated benzyne. A mechanism comprising domino transformation was suggested, and the structure of one key product was confirmed by a single crystal X-ray diffraction analysis.