Synthesis of the first examples of A-C8/C-C2 amide-Linked pyrrolo[2,1-c][1,4]benzodiazepine dimers

We report the synthesis of novel A-C8/C-C2 amide-linked pyrrolo[2,1-c][1,4]benzodiazepine dimers (4a and 4b) via convergent routes. These compounds lack the potent DNA interstrand cross-linking ability and resultant pronounced cytotoxicity of the known A-C8/A-C8′ linked dimers (e.g., 2a–b).