The inclusion of [1.1.1]bicyclopentanes as a bioisostere for aryl groups in pharmaceuticals has become increasingly prevalent in drug discovery. As a result, numerous recent methodologies have been developed to enable synthetic access to BCP containing motifs. Among these, there exist few known routes to BCP-containing pyrazoles (BCPP’s), which is a limitation due to the prevalence of arylpyrazoles in drugs and biologically active compounds. Our work has focused on developing new scaleable and short routes to access new BCPP’s from known, readily available precursors to enable scale-up of BCPP-containing compounds for drug discovery. This talk will detail the development, optimization and application of these methods to the synthesis of new compounds.

Development of scaleable methodologies to access a variety of substituted [1.1.1]bicyclopentane pyrzoles (BCPP’s) for drug discovery.

ACS Spring 2022

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