2-Ethylpyridine transition from medicinal chemistry to process chemistry requires an understanding of the solubility of impurities, key intermediates, and final product. The goal of process chemistry is to develop a robust and reliable streamlined process from the starting materials that are easily obtained to the final product. The final-product polymorph form and particle-size properties are dictated by the final step of product isolation. The final-product isolation step often involves recrystallization as the workup conditions. The workup conditions and subsequent fine-tuning of the conditions must be completely understood for material scale-up. In addition to the issue of scalability, efficient method transfer processes are involved with facilities responsible for scale-up (i.e., kilo labs, pilot plants). And now, with the need to understand the workup conditions earlier in the discovery cycle, analytical chemists are responsible for the decision-support process with medicinal and process chemistry. The batch-to-batch variability that is often observed with the scale-up from a medicinal chemistry bench to process chemistry can significantly affect the polymorphic forms and inherent solubility. As a result, the salt-selection process is often used as a tool to increase the solubility of the drug substance.
Was this article helpful?