Title:
METHOD FOR PREPARING DROXIDOPA AND INTERMEDIATE THEREOF
Document Type and Number:
WIPO Patent Application WO/2018/090670
Kind Code:
A1
Abstract:
The present invention relates to a method for preparing a droxidopa intermediate (2S,3R)-3-(3,4-dibenzyloxyphenyl)-2-dibenzylamino-3-hydroxypropionate, comprising carrying out asymmetric hydrogenation to 3-(3,4-dibenzyloxyphenyl)-2-dibenzylamino-3-oxo-propionate in an organic solvent under the catalysis of a ruthenium catalyst in the presence of a hydrogen donor reagent and an organic base. The reaction highly stereoselectively introduces two chiral centres of droxidopa in a high yield in one step. Furthermore, on the basis of the reaction, a method for preparing droxidopa is designed. The method has a simple and short process, and can stereoselectively synthesize droxidopa.
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Inventors:
SUN GUODONG (CN)
WANG ZHONGQING (CN)
WANG HAILONG (CN)
ZHOU ZIHONG (CN)
XU YONGBO (CN)
LUO ZHONGHUA (CN)
WANG ZHONGQING (CN)
WANG HAILONG (CN)
ZHOU ZIHONG (CN)
XU YONGBO (CN)
LUO ZHONGHUA (CN)
Application Number:
PCT/CN2017/095604
Publication Date:
May 24, 2018
Filing Date:
August 02, 2017
Export Citation:
Assignee:
SUNSHINE LAKE PHARMA CO LTD (CN)
International Classes:
C07C229/36; C07C227/16
Foreign References:
| JPS61251648A | 1986-11-08 | |||
| JPS61289067A | 1986-12-19 |
Other References:
WANG, YANZHAO ET AL.: "Synthesis of Chiral gamma-Amino Alcohols via a RuPHOX-Ru Catalyzed Asymmetric Hydrogenation of beta-Imide Ketones", CHINESE JOURNAL OF ORGANIC CHEMISTRY, vol. 34, no. 9, 23 May 2014 (2014-05-23), pages 1766 - 1772
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