Process Research & Development at Merck & Co., Inc. encompasses a number of diverse research groups whose focus ranges from enabling discovery chemistry (Discovery Process Chemistry), to discovery of new & innovative technologies (Enabling Technologies), to developing the ideal process for a manufacturing route (Process Chemistry). This presentation will highlight several short stories exemplifying my innovative work across multiple phases of development that benefitted multiple therapeutic areas ranging from antivirals to neuroscience. It will include the discovery and development of a palladium-catalyzed α-arylation of cyclopropyl nitriles and its application to open up new chemical space in various discovery programs, highlighting Discovery Process Chemistry’s impact in Discovery Chemistry, as well as the power or our Enabling Technologies group. Moving into early development, a novel direct and chemoselective 3’-phosphoramidation and its successful application to multi-kilo GMP campaigns will be presented, along with our work toward understanding the mechanism behind this unexpected selectivity. Lastly, I will share recent work as a team lead focused on developing an “ideal” manufacturing process for a marketed Active Pharmaceutical Ingredient.

Vignettes in process chemistry spanning enabling discovery chemistry to manufacturing route development

256th National Meeting (2018)

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