HTE Chemistry to Accelerate Medicinal Chemistry Programs

High-throughput experimentation (HTE) has emerged as a powerful tool in medicinal chemistry to accelerate drug discovery programs by rapidly screening and optimizing reaction conditions. In this poster, we will highlight the work of the SynTech Catalysis Laboratory, which specializes in HTE reaction condition screenings to remove synthetic bottlenecks throughout the medicinal chemistry portfolio within the Global Discovery Chemistry (GDC) organization of Novartis Biomedical Research. Our lab specializes in the optimization of metal-catalyzed reactions commonly encountered in drug discovery programs, including metal-catalyzed cross-coupling reactions, hydrogenations, carbonylations, and asymmetric hydrogenations.

We developed automated workflows and advanced crude analytical techniques to be able to rapidly screen many reaction conditions in parallel, allowing for systematic and efficient optimization of reaction parameters, such as catalysts, ligands, bases, solvents, and additives. This approach not only accelerates access to complex chemical matter for medicinal chemistry programs but also generates clean and reliable data for making informed decisions in the subsequent reaction optimization stages. We introduce some case studies showcasing the successful application of our HTE approach in accelerating drug discovery programs, overcoming synthetic challenges, and improving the efficiency of medicinal chemistry efforts. In conclusion, our catalysis laboratory utilizes HTE chemistry as a powerful tool to accelerate medicinal chemistry programs by systematically screening and optimizing reaction conditions, resulting in more efficient and streamlined drug discovery efforts within Novartis Biomedical Research, Global Discovery Chemistry organization.