In modern drug discovery projects, the synthetic chemistry team faces a constant tension between timely target delivery, investigation of new synthetic space and the optimization of the synthetic sequence used to deliver those compounds. In Pfizer Worldwide Medicinal Chemistry, a small team was charged with the specific role of optimizing bottleneck reaction steps to enable compound scale up and high speed analog synthesis. The presentation advocates for the employment of dedicated synthetic excellence teams in drug discovery projects through short examples of optimization work completed for the Mineralocorticoid Receptor, Ghrelin, Glucokinase Activator projects in CVMED, and Monocarbam project in the Antibacterials therapeutic area. Within the discussion, the talk shares the techniques used and lessons learnt from the successful execution of these optimization projects.

Building a successful reaction optimization group in drug discovery: Lessons learnt from Pfizer Worldwide Medicinal Chemistry

246th National Meeting (2013)

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