Synthesis of Isoquinoline from Benzimidates via Ru(II)-Catalyzed C-H Alkylation/Annulations with Diazo Compounds

A Ru(II)-catalyzed C-H alkylation/annulations of benzimidate with diazo compounds have been developed for the synthesis of functionalized isoquinoline. The reaction proceeds under mild condition and exhibit broad functional group tolerance. This strategy also provides a direct approach to isoquinolines and 3,4-dihydrophenanthridin synthesis. Moreover, Ru(II)-catalyzed C-H carbenoid functionalization of benzimidate with diazodiester is also demonstrated.