A CAPECITABINE HYDROXYL-DERIVATIVE, ITS PREPARATION PROCESSES AND USES FOR PREPARING CAPECITABINE

Title:

A CAPECITABINE HYDROXYL-DERIVATIVE, ITS PREPARATION PROCESSES AND USES FOR PREPARING CAPECITABINE

Document Type and Number:

WIPO Patent Application WO/2009/082844

Kind Code:

A1

Abstract:

A capecitabine hydroxyl-derivative as the following structure, its preparation processes and intermediates in the processes, and the use of hydrolyzing the said capecitabine hydroxyl-derivative to get capecitabine. The capecitabine hydroxyl-derivative provides the proper protecting group that can be removed by hydrolysis to get capecitabine under a weaker acidic or basic condition. The process of the reaction step is well controlled, the purity of the raw product is high and the resulting capecitabine meets the standard of US pharmacopoeia without complicated purification.

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Inventors:

JIANG XIANGRUI (CN)
CHEN WEIMING (CN)
HE XIUJUN (CN)
OU YANG (CN)
LIU ZHENG (CN)
ZHAO QINGJIE (CN)
SHEN JINGSHAN (CN)

Application Number:

PCT/CN2007/003871

Publication Date:

July 09, 2009

Filing Date:

December 28, 2007

Export Citation:

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Assignee:

TOPHARMAN SHANGHAI CO LTD (CN)
SHANGHAI INST MATERIA MEDICA (CN)
JIANG XIANGRUI (CN)
CHEN WEIMING (CN)
HE XIUJUN (CN)
OU YANG (CN)
LIU ZHENG (CN)
ZHAO QINGJIE (CN)
SHEN JINGSHAN (CN)

International Classes:

C07H19/06

Foreign References:

CN1896089A	2007-01-17
CN1201037A	1998-12-09
CN1126726A	1996-07-17
CN1660819A	2005-08-31

Other References:

YU JIANXIN ET AL.: "Improved Synthesis of Anticancer Drug Capecitabine.", CHINESE JOURNAL OF MEDICINAL CHEMISTRY, vol. 15, no. 3, June 2005 (2005-06-01), pages 173 - 176, XP008156583

Attorney, Agent or Firm:

KINGSOUND & PARTNERS (Block B Kingsound International Center, 116 Zizhuyuan Road, Haidian District, Beijing 7, CN)

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