In the pharmaceutical industry, an organic chemist must be adaptable to consistently fulfill development needs as a project advances from an early stage to selection of a compound for first-in-human clinical trials. Early in the research phase, value is added by developing library-amenable methods to open up new design space. As advanced lead matter is discovered, a synthetic chemists’ role changes to development of novel, yet practical syntheses of key compounds and intermediates that translate to larger scales to allow important clinical questions to be addressed. Case studies drawing from several drug discovery programs at Pfizer will be discussed including the decision-making that went into the selection of routes for Acetyl CoA-Carboxylase (ACC) Inhibitors, Ketohexokinase (KHK) inhibitors, and Adenosine Monophosphate-activated Protein Kinase (AMPK) Activators.

Speed to clinic: The critical role of organic synthesis in medicinal chemistry

256th National Meeting (2018)

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