THE PREPARATION METHOD AND INTERMEDIATES OF CAPECITABINE

WIPO Patent Application WO/2008/144980

A1

The present invention relates to the preparation method and intermediates of capecitabine. The present invention provides a new synthesis route for capecitabine, in which doxifluridine is used as the starting material and capecitabine is obtained through three steps of reaction. The present invention also provides the intermediates in the said synthesis route. The synthesis has short route, which can avoid producing stereoisomers. The method has a high yield, the technical process is easy to control and the quality of the products is stable.

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JIANG, Xiangrui (1088 Chuansha Road, Pudong, Shanghai 9, 201209, CN)
蒋翔锐 (中国上海市浦东新区川沙路1088号, Shanghai 9, 201209, CN)
OU, Yang (1088 Chuansha Road, Pudong, Shanghai 9, 201209, CN)

CN2007/070051

December 04, 2008

May 25, 2007

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TOPHARMAN SHANGHAI CO., LTD. (1088 Chuansha Road, Pudong, Shanghai 9, 201209, CN)
上海特化医药科技有限公司 (中国上海市浦东新区川沙路1088号, Shanghai 9, 201209, CN)
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES (No. 555, Zuchongzhi Road Pudong, Shanghai 3, 201203, CN)
中国科学院上海药物研究所 (中国上海市浦东张江祖冲之路555号, Shanghai 3, 201203, CN)
JIANG, Xiangrui (1088 Chuansha Road, Pudong, Shanghai 9, 201209, CN)

C07H19/073; C07H19/00

BEIJING HUIZE INTELLECTUAL PROPERTY LAW LLC (18A13, Horizon International Tower No. 6 Zhichun RoadHaidian District, Beijing 8, 100088, CN)

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