(2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone and preparation method and use thereof

US9376410B2 · kind B2 · utility

Assignees

• TOPHARMAN SHANGHAI CO., LTD. · CN
• SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES · CN
• TOPHARMAN SHANDONG CO., LTD. · CN

Inventors

• Guan Wang · Shanghai, CN
• Xiangrui Jiang · Shanghai, CN
• Xudong Gong · Ningbo City, CN
• Weiming Chen · Shanghai, CN
• Fuqiang Zhu · Shanghai, CN
• Rongxia Zhang · Shanghai, CN
• Xianguo Zhao · Shanghai, CN

Key dates

• Filing date: Oct 10, 2013
• Grant date: Jun 28, 2016
• Expiry date: Oct 10, 2033

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D413/12
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

This invention disclose (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone in a single configuration and preparation method and use thereof. The (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone, or a pharmaceutically acceptable salt, an ester, a prodrug or a solvate thereof according to the invention are important intermediates of a variety of anti-viral and anti-tumor active ingredients. A compound obtained from (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone via an acylation reaction can be directly used for preparing various anti-viral and anti-tumor drugs. The Chiral synthesis method and the spontaneous resolution method of the compound of (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone according to the invention have the following advantages: the reaction routes are short and simple with high yield and low cost, which are suitable for industrial application.