Process for the preparation of key intermediates of omarigliptin

US9481680B2 · kind B2 · utility

Assignee

• F.I.S. Fabbrica Italiana Sintetici S.p.A. · IT

Inventors

• Ottorino De Lucchi · Montecchio Maggiore, IT
• Enrico Rosso · Venezia, IT
• Simone Zaramella · Campodarsego, IT
• Stefano Tartaggia · Vicenza, IT

Key dates

• Filing date: Jan 19, 2015
• Grant date: Nov 1, 2016
• Expiry date: Jan 19, 2035

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D309/14
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

An improved process for the preparation of a key intermediate for the synthesis of the active ingredient Omarigliptin is provided. The key intermediate is a compound having the following formula (I)wherein R1 is propargyl or allyl group and P is an amine protecting group. The compound of formula (I) is prepared by converting a compound of formula (IV)by an amination reaction to a compound of formula (III),which is then protected to provide a compound of formula (II),which is then alkylated to provide the compound of formula (I).