During the course of an ongoing drug discovery project, access to previously unreported 2,5-disubstituted pyrazolo[4,3-c]cinnolin-3-ones was required with late stage substituent introduction at either the 2- or the 5- position. Treating a readily prepared 4-thioxocinnoline ester with substituted hydrazines afforded late stage access to the 2-position. Alternatively, late stage substitution at the 5-position was achieved by alkylation of 4-hydrazonopyrazol-3-ones, followed by SNAr ring closure. These two complimentary strategies toward the construction of 2,5-disubstituted pyrazolo[4,3-c]cinnolin-3-ones are detailed herein.

Preparation of 2,5-disubstituted pyrazolo[4,3-c]cinnolin-3-ones

240th National Meeting (2010)

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