Process for the preparation of pharmaceutical intermediates

US8394993B2 · kind B2 · utility

Assignee

• EGIS GYOCYSZERGYAR NYILVANOSAN MUKODO RESZVENYTARSASAG · HU

Inventors

• Tibor Mezei · Budapest, HU
• Gyula Lukacs · Budapest, HU
• Eniko Molnar · Ayacucho, PE
• Jozsef Barkoczy · Budapest, HU
• Balazs Volk · Budapest, HU
• Marta Porcs-Makkay · Bélapátfalva, HU
• János Szulágyi · Budapest, HU
• Mária Vajjon · Budapest, HU

Key dates

• Filing date: Nov 27, 2008
• Grant date: Mar 12, 2013
• Expiry date: Jun 4, 2029

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2601/02
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The invention relates to a process for the preparation of cyclopropyl benzyl ketone compounds of formula (II) wherein R1 represents fluorine or chlorine atom or C1-4 alkoxy group, by the reaction of a Grignard reagent, obtained from the reaction of compound of formula (V), wherein X represents chlorine or fluorine atom, with the compound of formula (IV), wherein R2 represents C1-4 alkyl group, having a straight or branched chain. The process can be applied preferably on industrial scale. Compound of formula (II), wherein R represents a fluorine atom in position 2 is an intermediate of the preparation process of prasugrel, which is a platelet inhibitor used in the therapy.