Process for the palladium-catalyzed coupling of terminal alkynes with aryl tosylates

US8487109B2 · kind B2 · utility

Assignee

• Sanofi · FR

Inventors

• Omar Rkyek · Tangier, MA
• Marc Nazare · Idstein, DE
• Andreas Lindenschmidt · Bad Soden, DE
• Matthias Urmann · Eschborn, DE
• Nis Halland · Frankfurt am Main, DE
• Jorge Alonso · Mannheim, DE

Key dates

• Filing date: Dec 23, 2009
• Grant date: Jul 16, 2013
• Expiry date: Aug 25, 2031

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2601/16
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The present invention relates to a process for the regioselective synthesis of compounds of the formula (I),wherein R1; R2; R3; R4; R5; J and W have the meanings indicated in the claims. The present invention provides an efficient and general palladium-catalyzed coupling process for aryl tosylates with terminal alkynes to a wide variety of substituted, multifunctional aryl-1-alkynes of the formula I.