Method for the preparation of oxazoles by condensing aromatic aldehydes with α-ketoximes to form n-oxides and reacting same with activated acid derivatives

US7544809B2 · kind B2 · utility

Assignee

• Sanofi-Aventis Deutschland GMBH · DE

Inventors

• Wolfgang Holla · Kelkheim, DE
• Rolf-Ludwig HOERLEIN · Frankfurt am Main, DE
• Berndt Kulitzscher · Esselbach, DE
• Wolfgang Laux · Paris, FR
• Thomas Stuedemann · Kelkheim, DE
• Christoph Tappertzhofen · Frankfurt, DE
• Robert J. H. Scheffer · Ingelheim am Rhein, DE

Key dates

• Filing date: May 29, 2007
• Grant date: Jun 9, 2009
• Expiry date: May 29, 2027

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P3/00
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The present invention is comprised of improved methods in the preparation of oxazoles which results in higher yields with less impurities and contaminants. Oxazoles constitute valuable intermediates in the synthesis of pharmaceutically active substances such as, for example peroxisome proliferator activated receptor (PPAR) agonists which are pharmaceutical actives which can have a positive influence on both lipid and glucose metabolism.