Title:
METHOD FOR PREPARING BICALUTAMIDE
Document Type and Number:
WIPO Patent Application WO/2022/083082
Kind Code:
A1
Abstract:
The present invention provides a method for preparing bicalutamide intermediate 2, comprising the following steps: dissolving N-[4-cyano-3-(trifluoromethyl)phenyl]-2-methacrylamide in a lower fatty acid ester solvent, successively adding sodium percarbonate and acetic anhydride, stirring, heating, and performing an epoxidation reaction to obtain a reaction solution; filtering the reaction solution, washing the organic phase with a sodium thiosulfate solution, and recovering the solvent under reduced pressure; and adding petroleum ether, and carrying out cooling, crystallizing, filtering and drying to obtain the bicalutamide intermediate 2. The method for preparing bicalutamide intermediate 2 has mild reaction conditions, high reaction yield and high epoxidation efficiency, and the reaction solvent can be recycled.
Inventors:
TANG BAOQING (CN)
ZHANG BANGLI (CN)
FU ZHIMING (CN)
FU ZHIXIONG (CN)
LIU HONGSHENG (CN)
XU GUOPING (CN)
ZHANG BANGLI (CN)
FU ZHIMING (CN)
FU ZHIXIONG (CN)
LIU HONGSHENG (CN)
XU GUOPING (CN)
Application Number:
PCT/CN2021/088332
Publication Date:
April 28, 2022
Filing Date:
April 20, 2021
Export Citation:
Assignee:
HUAIHUA BAOHUA BIOTECHNOLOGY CO LTD (CN)
International Classes:
C07C315/00; C07D303/48; C07C317/46; C07D301/12
Domestic Patent References:
| WO2016079521A1 | 2016-05-26 | |||
| WO2004039791A1 | 2004-05-13 |
Foreign References:
| CN112159372A | 2021-01-01 | |||
| CN101801945A | 2010-08-11 | |||
| CN1422853A | 2003-06-11 |
Other References:
CHEN BANG-CHI, ZHAO RULIN, GOVE STACEY, WANG BEI, SUNDEEN JOSEPH E., SALVATI MARK E., BARRISH JOEL C.: "Nucleophilic Aromatic Substitution of Methacrylamide Anion and Its Application to the Synthesis of the Anticancer Drug Bicalutamide", THE JOURNAL OF ORGANIC CHEMISTRY, AMERICAN CHEMICAL SOCIETY, vol. 68, no. 26, 1 December 2003 (2003-12-01), pages 10181 - 10182, XP055923432, ISSN: 0022-3263, DOI: 10.1021/jo035377c
Attorney, Agent or Firm:
BEIJING GAOWO LAW FIRM (CN)
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