Title:
METHOD FOR PREPARING SACUBITRIL INTERMEDIATE
Document Type and Number:
WIPO Patent Application WO/2019/019795
Kind Code:
A1
Abstract:
Disclosed in the present invention is a synthesis method for a sacubitril intermediate, the synthesis method belonging to the chemical-pharmaceutical field and comprising the following steps: performing a reaction of glycine and di-tert-butyl dicarbonate as starting materials under alkaline conditions, to effect dehydrogenation and amino protection, then performing substitution, deprotection and salification by means of a "one-pot method" with a compound of formula II under the action of a chiral catalyst, so as to obtain a chiral intermediate compound of formula III. The compound of formula III is reduced, refined and salified to obtain a compound of formula IV, and the compound of formula IV and di-tert-butyl carbonate are subjected to amino protection to produce a target product (R)-tert-butyl (1-([1,1'-biphenyl]-4-yl)-3-hydroxypropane-2-yl)carbamate of formula I. The raw materials and reagents required for the synthesis method of the sacubitril intermediate provided in the present invention are easily obtained, the reaction conditions are mild, the overall yield is high, the cost is low, just two salification processes are needed to complete the refining process, the post-treatment operation is simple, and the product quality is reliable and stable, the whole process being very suitable for industrial production.
Inventors:
XUE YI (CN)
WU SIQING (CN)
XU QIANG (CN)
HUANG SHUANG (CN)
LI WEISI (CN)
YANG JIAN (CN)
WU SIQING (CN)
XU QIANG (CN)
HUANG SHUANG (CN)
LI WEISI (CN)
YANG JIAN (CN)
Application Number:
PCT/CN2018/089113
Publication Date:
January 31, 2019
Filing Date:
May 31, 2018
Export Citation:
Assignee:
JIANGSU ZHONGBANG PHARMACEUTICAL CO LTD (CN)
International Classes:
C07C269/04; C07C271/16
Domestic Patent References:
| WO2016199688A1 | 2016-12-15 | |||
| WO2014032627A1 | 2014-03-06 | |||
| WO2016180275A1 | 2016-11-17 |
Foreign References:
| CN107382779A | 2017-11-24 | |||
| CN105330569A | 2016-02-17 | |||
| CN105985225A | 2016-10-05 |
Attorney, Agent or Firm:
NANJING ZHISHI LAW FIRM OF INTELLECTUAL PROPERTY (CN)
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