Synthesis and Reactivity of Azepino[3,4-b]indol-5-yl Trifluoromethanesulfonate

A convenient method for the synthesis of 5-substituted azepino[3,4-b]indol-1-ones 18–27 is described. This synthesis was based on palladium mediated cross-coupling reactions of the key intermediate azepino[3,4-b]indol-5-yl trifluoromethanesulfonates 3, obtained from the corresponding azepino[3,4-b]indole-1,5-dione 4.