Methods for the preparation of 5-[2-[7 (trifluoromethyl)-5-[4-(trifluoromethyl)phenyl]pyrazolo [1,5-A]pyrimidin-3-yl[ethynyl]-2-pyridinamine

US9447099B2 · kind B2 · utility

Assignee

• Hoffmann-La Roche Inc. · US

Inventors

• Stephan Bachmann · Allschwil, CH
• Daniel Bailey · Buffalo, US
• Jodie Brice · Florence, US
• Miall Cedilote · Florence, US
• Zhiming Dong · Florence, US
• Stefan Hildbrand · Riehen, CH
• Doreen Miller · Florence, US
• Paul Spurr · Riehen, CH
• Amit Srivastava · Aiken, US
• Juergen Wichmann · Basel, CH
• Thomas Woltering · Freiburg (Elbe), DE
• Jason Yang · Pleasanton, US
• Pingsheng Zhang · Millbrae, US

Key dates

• Filing date: Sep 27, 2012
• Grant date: Sep 20, 2016
• Expiry date: Mar 3, 2034

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y02P20/55
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The present invention provides methods for preparing 5-[2-[7-(trifluoromethyl)-5-[4-(trifluoromethyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]ethynyl]-2-pyridinamine (compound A), which is useful for the treatment of depression and other CNS disorders. The present methods are useful for preparing compound A on large scale in manufacturing facilities.