Process and intermediates for the preparation of imidazolidinone &agr;v integrin antagonists

US6407241B1 · kind B1 · utility

Assignee

• MERCK & CO., INC. · US

Inventors

• Mark S. Jensen · Wake Forest, US
• Michael Palucki · Fryeburg, US
• Nelo Rivera · Scotch Plains, US
• Kenneth M. Wells · Somerville, US
• Yi Xiao · Fanwood, US
• Yaling Wang · Westfield, US
• Chunhua Yang · Hunan, CN
• Nobuyoshi Yasuda · Mountainside, US

Key dates

• Filing date: Nov 7, 2000
• Grant date: Jun 18, 2002
• Expiry date: Nov 7, 2020

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D471/04
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

A novel process is provided for the preparation of imidazolidinone &agr;v&bgr;3/&agr;v&bgr;5 integrin antagonists, and the useful intermediates obtained therein. These compounds are antagonists of &agr;v&bgr;3/&agr;v&bgr;5 integrin receptors and thus useful for inhibiting bone resorption and treating and preventing osteoporosis. Also disclosed is 3-{2-oxo-3-[3-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-propyl]imidazolidin-1-yl}-3(S)-(6-methoxy-pyridin-3-yl)-propionic acid in the form of a hemihydrate.