Journal
ORGANIC PROCESS RESEARCH & DEVELOPMENT
Volume 22, Issue 7, Pages 898-902Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.oprd.8b00080
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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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