Synthesis of the Hydrazinyl Pyridine Intermediate: Phase-Appropriate Delivery

Autor: Andrew Cosbie, Steven M. Mennen, Ashraf Wilsily, Jacqueline E. Milne
Rok vydání: 2017
Předmět:
Zdroj: Organic Process Research & Development. 21:1286-1293
ISSN: 1520-586X
1083-6160
DOI: 10.1021/acs.oprd.7b00172
Popis: A two-step synthesis of an intermediate for a drug-candidate, 3-fluoro-2-hydrazinyl-5-(1-methyl-1H-pyrazol-4-yl)pyridine (1), was developed and optimized according to the strategic priorities of the program. The bond disconnection remained unchanged from the initial route to the scale-up routes; however, the process evolved as the program’s priorities progressed. Speed, securing the raw material supply chain, and cost were all factors considered during development. The strategies to enable multikilogram deliveries are highlighted in this report.
Databáze: OpenAIRE