Discovery of drug candidates can benefit greatly from early identification and resolution of chemistry bottlenecks which can improve speed of execution of SAR, breadth of chemical space explored, and rapidity in transition to development of high quality candidates. In response, we have established Discovery teams integrating traditional medicinal and process chemistry mindsets, as a way to augment synthetic chemistry capabilities and expertise. This talk will highlight specific areas in which this guiding principal has been applied by the Discovery Process Chemistry (DPC) group at Merck, focusing on the development and application of a unique palladium-catalyzed alpha-arylation strategy to access small-ring systems containing bulky groups vicinal to the site of bond formation.

Discovery of a novel alpha-arylation reaction and the importance of synthetic innovations in drug discovery and development

256th National Meeting (2018)

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