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One-pot directed alkylation/deprotection strategy for the synthesis of substituted pyrrole[3,4-d]pyridazinones. 2015

Reji N Nair, and Thomas D Bannister
The Scripps Research Institute, 130 Scripps Way, Jupiter, FL 33418, http://www.scripps.edu/research/faculty/bannister.

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.

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