3-alkyl-5- (4-alkyl-5-oxo-tetrahydrofutran-2-yl) pyrrolidin-2-one derivatives as intermediates in the synthesis of renin inhibitors

US8198465B2 · kind B2 · utility

Assignee

• Novartis AG · CH

Inventors

• Gottfried Sedelmeier · Schallstadt, DE
• Dominique Grimler · Basel, CH
• Murat Acemoglu · Basel, CH

Key dates

• Filing date: Jun 25, 2010
• Grant date: Jun 12, 2012
• Expiry date: Sep 28, 2030

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y02P20/55
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a compound of the formula II,or a salt thereof, and a compound of formula VIor a salt thereof, wherein R3 and R4 as well as Act are as defined in the specification, and processes of manufacturing these.Additionally transformation of compounds (VI) with metallo organic compounds (VII) give rise to the new compounds (VIII) which are direct precursors for the preparation of Aliskiren.