Title:
METHOD FOR PREPARING NINTEDANIB AND INTERMEDIATE THEREOF
Document Type and Number:
WIPO Patent Application WO/2018/068733
Kind Code:
A1
Abstract:
The present invention provides a method for preparing nintedanib. The method of the present invention is carried out by using 4-halo-3-nitro-benzoic acid methyl ester (compound II) and 3-oxo-3-phenylpropionate (compound III) as raw materials, and preparing nintedanib via intermediates of 4-(1-alkoxy-1,3-dioxo-3-phenylpropan-2-yl)-3-nitrobenzoic acid methyl ester (compound IV) and 3-benzoyl-2-oxoindoline-6-methyl formate (compound V). The method for preparing nintedanib (I) provided by the invention has the advantages of using easily obtained raw materials, having a simple process, being cost effective and environmentally friendly, and is suitable for industrial-scale production.
Inventors:
LI ZENG (CN)
CHENG XIAOSONG (CN)
HE XIANLIANG (CN)
ZHANG JICHENG (CN)
HUANG LUNING (CN)
TAO ANPING (CN)
GU HONG (CN)
CHENG XIAOSONG (CN)
HE XIANLIANG (CN)
ZHANG JICHENG (CN)
HUANG LUNING (CN)
TAO ANPING (CN)
GU HONG (CN)
Application Number:
PCT/CN2017/105723
Publication Date:
April 19, 2018
Filing Date:
October 11, 2017
Export Citation:
Assignee:
ZHEJIANG HUAHAI PHARMACEUTICALS CO LTD (CN)
SHANGHAI SYNCORES TECH INC (CN)
SHANGHAI SYNCORES TECH INC (CN)
International Classes:
C07D209/34; C07C201/12; C07C205/61
Domestic Patent References:
| WO2016178064A1 | 2016-11-10 | |||
| WO2012068441A2 | 2012-05-24 |
Foreign References:
| CN105461609A | 2016-04-06 | |||
| CN101883756A | 2010-11-10 | |||
| CN104262232A | 2015-01-07 |
Other References:
LIU, WEI ET AL.: "Graphical Synthetic routes to Nintedanib", CHINESE JOURNAL OF MEDICINAL CHEMISTRY (NON-OFFICIAL TRANSLATION), vol. 26, no. 2, 30 April 2016 (2016-04-30), pages 154 - 156
Attorney, Agent or Firm:
BOSS & YOUNG PATENT AND TRADEMARK LAW OFFICE (CN)
Download PDF: