Synthesis of 4-substituted azepino[3,4-b]indole-1,5-diones

Mono- or dibromo derivatives and were prepared by an efficient two-step route from 10-methyl-azepino[3,4-b]indole-1,5-dione . Elimination reaction on gave access to 4-bromo-10-methyl-2H,10H-azepino[3,4-b]indole-1,5-diones . Finally, 4-substituted 10-methyl-2H,10H-azepino[3,4-b]indole-1,5-diones were synthesised in good yields from via palladium-mediated cross-coupling reactions.