Title:
METHOD FOR SYNTHESIZING NIRMATRELVIR INTERMEDIATE
Document Type and Number:
WIPO Patent Application WO/2023/216317
Kind Code:
A1
Abstract:
Provided is a method for synthesizing a nirmatrelvir intermediate in formula (III), specifically comprising: (1) dissolving a compound represented by formula V in a solvent, and reacting with trifluoromethanesulfonic anhydride under an alkaline condition to give a compound represented by formula VI; and (2) adding DBU to the compound represented by formula VI for an elimination reaction to give a product represented by formula III. The method features cost-efficiency, a stable process, and a high purity and high yield of the synthesized product, and is suitable for industrial production.
Inventors:
LIU GUOJIE (CN)
HU YIFANG (CN)
TIAN XIANGYIN (CN)
WANG PENG (CN)
ZHANG WENLING (CN)
QIAN GANG (CN)
HU YIFANG (CN)
TIAN XIANGYIN (CN)
WANG PENG (CN)
ZHANG WENLING (CN)
QIAN GANG (CN)
Application Number:
PCT/CN2022/094641
Publication Date:
November 16, 2023
Filing Date:
May 24, 2022
Export Citation:
Assignee:
HANGZHOU GUORUI BIO TECH CO LTD (CN)
International Classes:
C07D207/16
Foreign References:
| CN114085180A | 2022-02-25 | |||
| CN114436929A | 2022-05-06 | |||
| EP3854783A1 | 2021-07-28 | |||
| CN104379576A | 2015-02-25 | |||
| US20210171520A1 | 2021-06-10 | |||
| CN114057627A | 2022-02-18 | |||
| CN114133350A | 2022-03-04 |
Other References:
KYU-YOUNG KIM, BONG CHAN KIM, HEE BONG LEE, HYUNIK SHIN: "Nucleophilic Fluorination of Triflates by Tetrabutylammonium Bifluoride", THE JOURNAL OF ORGANIC CHEMISTRY, AMERICAN CHEMICAL SOCIETY, vol. 73, no. 20, 17 October 2008 (2008-10-17), pages 8106 - 8108, XP055012140, ISSN: 00223263, DOI: 10.1021/jo8015659
LIU TING; YAN NAN; ZHAO HUI; WANG ZHEN-XING; HU XIANG-GUO: "Synthesis and antibacterial activity of 6(R)- and 6(S)-fluoropenibruguieramine As: Fluorine as a probe for testing the powerfulness of memory of chirality (MOC)", JOURNAL OF FLUORINE CHEMISTRY, ELSEVIER, NL, vol. 207, 3 January 2018 (2018-01-03), NL , pages 18 - 23, XP085342988, ISSN: 0022-1139, DOI: 10.1016/j.jfluchem.2018.01.002
LIU TING; YAN NAN; ZHAO HUI; WANG ZHEN-XING; HU XIANG-GUO: "Synthesis and antibacterial activity of 6(R)- and 6(S)-fluoropenibruguieramine As: Fluorine as a probe for testing the powerfulness of memory of chirality (MOC)", JOURNAL OF FLUORINE CHEMISTRY, ELSEVIER, NL, vol. 207, 3 January 2018 (2018-01-03), NL , pages 18 - 23, XP085342988, ISSN: 0022-1139, DOI: 10.1016/j.jfluchem.2018.01.002
Attorney, Agent or Firm:
JJS INTELLECTUAL PROPERTY AGENCY LTD. (CN)
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