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.

JP6237237	Base part protection oligonucleotide
WO/2010/000459	CYCLOPROPYL POLYMERASE INHIBITORS
JPH03504492	[Title of the Invention] alpha ‐amino acyl group -- 5- and 3' -- a new derivative of - or 5'2 replaced in position of -' ‐Deoxy melon gin, a generation method for the same, and those existing medicines

JIANG XIANGRUI (CN)
OU YANG (CN)
SHEN JINGSHAN (CN)

PCT/CN2007/070051

December 04, 2008

May 25, 2007

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TOPHARMAN SHANGHAI CO LTD (CN)
SHANGHAI INST MATERIA MEDICA (CN)
JIANG XIANGRUI (CN)
OU YANG (CN)
SHEN JINGSHAN (CN)

C07H19/073

CN1935828A	2007-03-28
US5530110A	1996-06-25

DONG H. ET AL.: "Improved process for the synthesis of Doxifluridine", ZHONGGUO YIYAO GONGYE ZAZHI, vol. 33, no. 3, pages 108 - 109
DATABASE CHEMICAL ABSTRACTS [online] Database accession no. (128:213389)
YU J. ET AL.: "Improved synthesis of anticancer drug capecitabine", ZHONGGUO YAOWU HUAXUE ZAZHI, vol. 15, no. 3, June 2005 (2005-06-01), pages 173 - 175, 187

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