Palladium catalyzed indolization of 2-bromo or chloroanilines

US7126009B2 · kind B2 · utility

Assignee

• Boehringer Ingelheim International GmbH · DE

Inventors

• Guisheng Li · Richmond, US
• Jianxiu Liu · Richmond, US
• Zhi-Hui Lu · Glen Allen, US
• Frank Roschangar · Glen Allen, US
• Chris Hugh Senanayake · Brookfield, US
• Ming-Tung Shen · Guilford, US

Key dates

• Filing date: Mar 14, 2005
• Grant date: Oct 24, 2006
• Expiry date: May 20, 2025

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2601/04
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The present invention provides a method for making substituted indole compounds of general formula III comprising the step of:(a) reacting a 2-bromoaniline or 2-chloroaniline of general formula (I)(I)wherein: X, R and R1 are defined hereinwith a substituted acetylene of formula (II)wherein R2 and R3 are defined herein in the presence of a palladium catalyst, a ligand, and a base in a solvent at a suitable temperature to give a compound of formula (III);