Transition metal catalyzed synthesis of 2H-indazoles

US8283476B2 · kind B2 · utility

Assignee

• Sanofi · FR

Inventors

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

Key dates

• Filing date: Dec 22, 2009
• Grant date: Oct 9, 2012
• Expiry date: Jun 2, 2030

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P33/14
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to a process for the regioselective synthesis of compounds of the formula I,wherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct transition metal catalyzed process to a wide variety of multifunctional 2H-indazoles or 2H-azaindazoles of the formula (I) from 2-halo-phenylacetylenes or (2-sulfonato)phenylacetylenes and monosubstituted hydrazines.