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Title:
7-KETOLITHOCHOLIC ACID INTERMEDIATE, SYNTHESIS METHOD THEREFOR, AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2023/179721
Kind Code:
A1
Abstract:
The present invention provides a synthesis method for a 7-ketolithocholic acid or an intermediate thereof, which is prepared from a new intermediate I-1. According to the method, phytosterol degradation product bisnoralchol is used as a starting material, and the 7-ketolithocholic acid or the intermediate thereof is obtained by means of an oxidation reaction, a Knoevenagel reaction (or wittig reaction), hydrogenation, a ketal protection reaction, an allylic oxidation reaction, ketal removal protection, and the hydrogenation. According to the method of the present invention, raw materials are readily available, the yield is high, reaction conditions are simple and mild, and the method is suitable for industrial production.

Inventors:
YANG YINGQUAN (CN)
YUAN HAITAO (CN)
ZHOU PANLONG (CN)
WANG FEI (CN)
WU HUCHENG (CN)
Application Number:
PCT/CN2023/083436
Publication Date:
September 28, 2023
Filing Date:
March 23, 2023
Export Citation:
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Assignee:
SUZHOU ENTECH NEW MATERIAL TECH CO LTD (CN)
International Classes:
C07J9/00; C07J5/00; C07J21/00
Domestic Patent References:
WO2022228080A12022-11-03
WO2022039983A22022-02-24
Foreign References:
CN115536719A2022-12-30
CN115181150A2022-10-14
CN107628962A2018-01-26
CN102286066A2011-12-21
CN103044514A2013-04-17
CN111560045A2020-08-21
Other References:
SAMAJA, GISELA A. ET AL.: "27-Nor-DELTA4-dafachronic Acid is a Synthetic Ligand of Caenorhabditis Elegans DAF-12 Receptor", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 23, no. 10, 28 March 2013 (2013-03-28), pages 2893 - 2896, XP028582269, ISSN: 0960-894X, DOI: 10.1016/j.bmcl.2013.03.071
Attorney, Agent or Firm:
BEIJING ORIGINTELLIGENCE IP LAW FIRM et al. (CN)
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