The chemical complexity and diversity of pharmaceutically active molecules presents a rich opportunity for application of modern catalysis. However, successfully adapting published catalytic methods to complex molecules requires the ability to simultaneously adjust multiple reaction parameters such as solvent, ligand, additives and metal source in a time- and material-sparing manner. To overcome these challenges, scientists at Merck have helped pioneer high-throughput experimentation (HTE) approaches to rapidly identify optimum catalysts and conditions customized for each transformation. Recent advances in HTE miniaturization, automation and analysis have greatly expanded the impact of catalysis in drug discovery.  Several case studies will be discussed that illustrate the diverse ways HTE can enable drug discovery, employing a wide variety of chemistries such as modern cross-coupling and C-H functionalization catalysis.

Leveraging high-throughput experimentation and cutting-edge synthetic chemistries to improve the quality and speed of the drug discovery design cycle

2019 Spring National Meeting

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