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A practical one-pot solid-phase parallel diversity-oriented synthesis (DOS) strategy has been successfully applied for the construction of scaffolds embedded with privileged pyrrolo [2,1-c][1,4]benzodiazepines (PBDs) and their dilactams. The synthetic approach involves AlCl 3 –NaI assisted cleavage of resin-bound ester, with amine coupling and tandem azido-reductive cyclization as the key...
A series of 1,2,3-triazole-containing pyrrolo[2,1-c][1,4]benzodiazepine dimers have been prepared efficiently by employing a ‘click’ chemistry protocol. This method involves 1,3-dipolar cycloaddition of terminal alkynes with organic azides using a Cu(I)-catalyst. Further, these molecules exhibited interesting DNA-binding affinity profiles.
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