Phosphine‐Catalyzed Domino Annulation Reactions of o‐Aminotrifluoroacetophenone Derivatives with Morita–Baylis–Hillman Carbonates: Construction of Tetrahydrofuro[3,2‐b]indolines

Abstract

AbstractThe domino annulation reactions of o‐aminotrifluoroacetophenone derivatives and MBH carbonates enabled by PPh3 have been reported, which provide a series of tetrahydrofuro[3,2‐b]indolines containing a CF3‐substituted tetrasubstituted carbon stereocenters in yields of 74 to 95% and >20:1 dr. In this process, MBH carbonates were used as C1/C3 synthons. The MTT assay shows that the products exhibit the activity of inhibitory effect on proliferation on Hela cancer cell line.