Title:
SYNTHESIS METHOD FOR PAXLOVID INTERMEDIATE
Document Type and Number:
WIPO Patent Application WO/2023/168827
Kind Code:
A1
Abstract:
The present invention relates to the technical field of chemical intermediates. Disclosed is a synthesis method for a paxlovid intermediate, comprising the following steps: reacting 3,3-dimethyl-4-oxobutyrate with S-substituted sulfinamide to generate a compound C-1; reacting the compound C-1 with monohalogen substituted acetate under the action of strong base, and using the chiral induction of S-substituted sulfinamide to obtain a compound C-2; the compound C-2 forming a transitional state intermediate compound C-3 under the action of the strong base, and further forming a compound C-4 under the action of the strong base and the chiral induction of S-substituted sulfinyl; removing a protecting group from the compound C-4 to obtain a compound C-5; and performing a reduction reaction on the compound C-5 to obtain the paxlovid intermediate. According to the method of the present invention, the raw materials are low in price and easy to obtain, the energy consumption is low, the operation is simple, the safety is high, and the loss caused by chiral resolution is reduced.
Inventors:
LIU GUOJIE (CN)
CHEN ZHENGSHU (CN)
TIAN XIANGYIN (CN)
WANG PENG (CN)
QIAN GANG (CN)
CHEN ZHENGSHU (CN)
TIAN XIANGYIN (CN)
WANG PENG (CN)
QIAN GANG (CN)
Application Number:
PCT/CN2022/093015
Publication Date:
September 14, 2023
Filing Date:
May 16, 2022
Export Citation:
Assignee:
HANGZHOU GUORUI BIO TECH CO LTD (CN)
International Classes:
C07D209/52; C07B53/00; C07C313/06; C07D203/24
Foreign References:
| CN1805931A | 2006-07-19 | |||
| CN101384551A | 2009-03-11 | |||
| CN114057627A | 2022-02-18 | |||
| CN103435532A | 2013-12-11 |
Attorney, Agent or Firm:
JJS INTELLECTUAL PROPERTY AGENCY LTD. (CN)
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