An Improved Process for the Preparation of a Covalent Kinase Inhibitor through a C–N Bond-Forming SNAr Reaction
2018
An improved API step for the formation of an aminopyrimidine-based kinase inhibitor is described. The presence of a reactive acrylamide functional group presented a considerable challenge during scale-up, resulting in side-product formation and low in-process yields for the final SNAr reaction. Impurity identification guided process development efforts, enabling rapid scale-up of a safe and phase-appropriate process to deliver the API to support toxicology studies.
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