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Title:
ESTRONE SYNTHESIS METHOD
Document Type and Number:
WIPO Patent Application WO/2023/126014
Kind Code:
A1
Abstract:
An estrone synthesis method. The method comprises the following steps: 1) performing aromatization reaction, uniformly mixing estra-4,9-diene-3,17-dione, acetic anhydride, and dichloromethane that serve as raw materials, adding acetyl bromide, then reacting under nitrogen protection, the reaction temperature being 0-50°C, the reaction time being 1-24 h, after the completion of the reaction, adding a lye to regulate the pH to 7-9, layering, and concentrating an organic phase to obtain an esterified product; and 2) performing hydrolysis reaction, adding methanol to disperse the esterified product, adding alkali, continuing the reaction, the reaction temperature being 0-50°C, the reaction time being 1-24 h, after the completion of the reaction, adding acid to neutralize, adding water to dilute, and filtering to obtain estrone.

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Inventors:
ZHANG ZHENGBIN (CN)
LI CHUN (CN)
YIN JINYU (CN)
ZHANG JIEFENG (CN)
LIU GUANGYUAN (CN)
WU JING (CN)
WU XIAOFANG (CN)
Application Number:
PCT/CN2023/074486
Publication Date:
July 06, 2023
Filing Date:
February 04, 2023
Export Citation:
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Assignee:
ZHEJIANG XIANJU JUNYE PHARMACEUTICAL CO LTD (CN)
JIANGXI JUNYE BIOLOGICAL PHARMACEUTICAL CO LTD (CN)
International Classes:
C07J1/00
Foreign References:
CN114315942A2022-04-12
US3117142A1964-01-07
CN102603840A2012-07-25
CN102675393A2012-09-19
CN105001293A2015-10-28
CN112225773A2021-01-15
Other References:
ADAM HENDRICKS J.; HANSON ROBERT N.; AMOLINS MICHAEL; MIHELCIC JOHN M.; BLAGG BRIAN S.: "Synthesis and preliminary evaluation steroidal antiestrogen–geldanamycin conjug", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, ELSEVIER, AMSTERDAM NL, vol. 23, no. 12, 4 April 2013 (2013-04-04), Amsterdam NL , pages 3635 - 3639, XP028543376, ISSN: 0960-894X, DOI: 10.1016/j.bmcl.2013.03.116
POUZAR VLADIMÍR, ČERNÝ IVAN, DRAŠAR PAVEL, HAVEL MIROSLAV: "New method of preparation of cardioglycoside hemisuccinates", COLLECTION OF CZECHOSLOVAK CHEMICAL COMMUNICATIONS, vol. 51, no. 9, 1 September 1986 (1986-09-01), pages 2019 - 2028, XP093075728, ISSN: 0010-0765, DOI: 10.1135/cccc19862019
Attorney, Agent or Firm:
TZIZHOU NANFANG TRADEMARK PATENT AGENCY CO., LTD (CN)
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