One-pot directed alkylation/deprotection strategy for the synthesis of substituted pyrrole[3,4-d]pyridazinones.

In the course of an SAR study of pyrrole[3,4-d]pyridazinones we optimized conditions for a one pot directed lithiation / alkylation reaction that also promoted in situ cleavage of a Boc-protecting group on the pyrrole ring. The efficiency of the process allowed access to a number of substituted analogues of interest as possible antitumor agents.