Title:
A PREPARATION METHOD OF 1-(4-FLUOROPHENYL)-(3R)-[3-(4-FLUOROPHENYL)-(3S)-HYDROXYPROPYL]-(4S)-(4-HYDROXYPHENYL)-2-AZETIDINONE
Document Type and Number:
WIPO Patent Application WO/2006/050634
Kind Code:
A1
Abstract:
An improved process for producing 1-(4-fluorophenyl)-(3R)-[3-(4-fluorophenyl)-(3S)-hydroxypropyl]-(4S)-(4-hydroxyphenyl)-2-azetidinone, comprising: cyclizing the β-(substituted-amino)amide of formula (I) in the presence of a inert organic solvent, a organic base, a fluoride ion catalyst cyclizing agent and a chiral structure protector while removing the protecting groups, and producing the object compound of formula (II). In particular, the chiral structure protector is chlorotrimethylsilane.
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Inventors:
GU LIANQUAN (CN)
RUAN JIWU (CN)
HUANG ZHISHU (CN)
RUAN JIWU (CN)
HUANG ZHISHU (CN)
Application Number:
PCT/CN2004/001292
Publication Date:
May 18, 2006
Filing Date:
November 15, 2004
Export Citation:
Assignee:
XIAMEN MCHEM PHARMA GROUP LTD (CN)
GU LIANQUAN (CN)
RUAN JIWU (CN)
HUANG ZHISHU (CN)
GU LIANQUAN (CN)
RUAN JIWU (CN)
HUANG ZHISHU (CN)
International Classes:
C07D205/08; (IPC1-7): C07D205/08
Foreign References:
| CN1329592A | 2002-01-02 | |||
| US5856473A | 1999-01-05 | |||
| US6093812A | 2000-07-25 |
Other References:
CAI ZHENGYAN ET AL: "Graphical Synthetic Routes of Enzetimibe.", CHINESE JOURNAL OF PHARMACEUTICALS., vol. 35, no. 4, April 2004 (2004-04-01), pages 251 - 253
Attorney, Agent or Firm:
SCIHEAD PATENT AGENT CO., LTD. (Huihua Commercial & Trade Building No.80,
XianLie Zhong Roa, Guangzhou Guangdong 0, CN)
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