At Pfizer, academic collaborations are an important driver for synthetic innovations and, by broadening the available toolkit for discovery synthesis, lead to faster delivery of analogs for SAR explorations. We seek robust synthetic transformations that use diverse monomer sets to provide a wide range of target molecules.  In this presentation, we will showcase a successful example of academic/industry partnership between Pfizer’s Medicine Design group and Hong Kong University of Science and Technology.  In this collaboration, an aza-Achmatowicz rearrangement followed by a Pd-catalyzed arylation reaction sequence was enabled. This novel method uses furfural, a commodity chemical and a broad range of boronic acids to deliver 2-aryl piperidine building blocks with substitution possible at all positions on the piperidine.

Academic collaborations at Pfizer: Synthesis of piperidine building blocks

ACS Spring 2022

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.