2R,4S,S,S- and 2S,4R,S,S-hydroxyitraconazole

US6455530B1 · kind B1 · utility

Assignee

• Sepracor, Inc. · US

Inventors

• Patrick Koch · Marlborough, US
• John Richard McCullough · Hudson, US
• Chris Hugh Senanayake · Brookfield, US
• Gerald J. Tanoury · Marlborough, US
• Yaping Hong · Framingham, US

Key dates

• Filing date: Sep 18, 2000
• Grant date: Sep 24, 2002
• Expiry date: Sep 18, 2020

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D249/12
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

A method of preparation of optically pure isomers of hydroxyitraconazole, in particular the two cis dioxolane diastereomers of the sec-butyl (S,S)-isomer, and to phosphate and sulfate derivatives thereof is disclosed. Pharmaceutical compositions containing these compounds and to their use for the treatment of fungal infection are also disclosed.