During the course of a drug discovery project, access to 2,5-disubstituted pyrazolo[4,3-c]quinolin-3-ones  and pyrazolo[4,3-c]cinnolin-3-ones was required with late stage substituent introduction at either the 2- or the 5-position.  Substituent introduction at the 2-position was achieved via the corresponding thioesters.  Access to substitution at the 5-position was achieved through a common orthogonal intermediate, 5-(2-fluorophenyl)-3-oxo-2,4-dihydro-3H-pyrazol-3-one. The synthetic approaches examined to and developed for the construction of these scaffolds will be detailed herein.

Synthetic approaches for the construction of 2,5-disubstituted pyrazolo[4,3-<i>c</i>]quinolin-3-ones and pyrazolo[4,3-<i>c</i>]cinnolin-3-ones

242nd National Meeting (2011)

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