Title:
A METHOD FOR THE PREPARATION OF DOCETAXEL, THE INTERMEDIATES AND THE PREPARATION METHODS THEREOF
Document Type and Number:
WIPO Patent Application WO/2010/057378
Kind Code:
A1
Abstract:
A method for the preparation of docetaxel of formula 1, comprising: (1) acylating the hydroxyl of compound 2 with compound 3 to obtain compound 4; (2) removing the hydroxyl-protecting group R1 of the obtained compound 4 to obtain compound 5; (3) removing one Boc group of compound 5 obtained in the step (2) to obtain compound 6; (4) removing Ac of compound 6 obtained in step (3) to obtain docetaxel of formula 1, in which R1 is tert-butyldimethylsilyl, triethylsilyl, ethoxyethyl, tetrahydropyranyl, trichloroethoxycarbonyl, or methoxymethyl. The intermediates used in the preparation of docetaxel and the preparation methods thereof.
Inventors:
SHEN XIN (CN)
ZHAN HUAXING (CN)
YANG JIDONG (CN)
HE XIAO (CN)
LIN FUXING (CN)
WU SHAOHONG (CN)
ZHAN HUAXING (CN)
YANG JIDONG (CN)
HE XIAO (CN)
LIN FUXING (CN)
WU SHAOHONG (CN)
Application Number:
PCT/CN2009/071939
Publication Date:
May 27, 2010
Filing Date:
May 22, 2009
Export Citation:
Assignee:
SHANGHAI PARLING PHARMA TECH C (CN)
SHEN XIN (CN)
ZHAN HUAXING (CN)
YANG JIDONG (CN)
HE XIAO (CN)
LIN FUXING (CN)
WU SHAOHONG (CN)
SHEN XIN (CN)
ZHAN HUAXING (CN)
YANG JIDONG (CN)
HE XIAO (CN)
LIN FUXING (CN)
WU SHAOHONG (CN)
International Classes:
C07C269/04; C07D305/14; C07C269/06; C07C271/22
Domestic Patent References:
| WO2008032104A1 | 2008-03-20 | |||
| WO2007073383A1 | 2007-06-28 |
Foreign References:
| CN1942460A | 2007-04-04 | |||
| CN101048394A | 2007-10-03 | |||
| CN101020673A | 2007-08-22 | |||
| US6900342B2 | 2005-05-31 | |||
| CN101343262A | 2009-01-14 |
Other References:
JOËLLE. DUBOIS ET AL.: "Conformation of Taxotere® and Analogues Determined by NMR Spectroscopy and Molecular Modeling Studies.", TETRAHEDRON, vol. 49, no. 30, 23 July 1993 (1993-07-23), pages 6533 - 6544
SHI, BING XING ET AL.: "Studies on the Quantitative Structure-activity Relationships of Paclitaxel Analogues.", CHEMICAL JOURNAL OF CHINESE UNIVERSITIES, vol. 21, no. 3, March 2000 (2000-03-01), pages 401 - 406
LI, CHUN BAO ET AL.: "Synthesis of Esters of Taxotere Side Chain.", CHEMICAL INDUSTRY AND ENGINEERING, vol. 18, no. 5, October 2001 (2001-10-01), pages 285 - 289
SHI, BING XING ET AL.: "Studies on the Quantitative Structure-activity Relationships of Paclitaxel Analogues.", CHEMICAL JOURNAL OF CHINESE UNIVERSITIES, vol. 21, no. 3, March 2000 (2000-03-01), pages 401 - 406
LI, CHUN BAO ET AL.: "Synthesis of Esters of Taxotere Side Chain.", CHEMICAL INDUSTRY AND ENGINEERING, vol. 18, no. 5, October 2001 (2001-10-01), pages 285 - 289
Attorney, Agent or Firm:
SHANGHAI ZHI XIN PATENT AGENT LTD. (Zhijun Buliding No. 1223 Xietu Road, Shanghai 2, CN)
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