Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
5268530 | Tetrahedron Letters | 2012 | 4 Pages |
Abstract
4-(4-Iodo-1H-pyrazol-1-yl)piperidine is a key intermediate in the synthesis of Crizotinib. We report a robust three-step synthesis that has successfully delivered multi-kilogram quantities of the key intermediate. The process includes nucleophilic aromatic substitution of 4-chloropyridine with pyrazole, followed by hydrogenation of the pyridine moiety and subsequent iodination of the pyrazole which all required optimization to ensure successful scale-up.
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Steven J. Fussell, Amy Luan, Philip Peach, Gemma Scotney,