Title:
SYNTHESIS METHOD FOR ESAXERENONE AND INTERMEDIATE THEREOF
Document Type and Number:
WIPO Patent Application WO/2023/035571
Kind Code:
A1
Abstract:
Provided is a new synthesis method for an intermediate of esaxerenone. The method comprises: (1) reacting 2-(trifluoromethyl)phenylacetic acid as a raw material with ethyl chloroformate or isobutyl chloroformate in an inert solvent in the presence of an alkali to produce a mixed anhydride, then reacting same with ammonia to obtain a corresponding amide compound of formula II; (2) subjecting the amide compound of formula II obtained in step (1) to a dehydration reaction in the presence of a dehydrating agent and an acid-binding agent to obtain an isocyanide compound of formula III; and (3) subjecting the isocyanide compound of formula III obtained in step (2) to a cyclization reaction with ethyl 2-butynonate in the presence of an alkali and a metal catalyst to form a pyrrole ring compound of formula IV; and the reaction equation is shown below: Compared to the prior art, the technical solution of the present invention has the advantages of a high yield, a simple post-treatment, low costs and easy industrialization, etc.
Inventors:
RUAN JING (CN)
ZHANG XINXIN (CN)
YAN GONGCHAO (CN)
RUAN XIAONA (CN)
ZHANG WEI (CN)
ZHANG XINXIN (CN)
YAN GONGCHAO (CN)
RUAN XIAONA (CN)
ZHANG WEI (CN)
Application Number:
PCT/CN2022/080532
Publication Date:
March 16, 2023
Filing Date:
March 13, 2022
Export Citation:
Assignee:
SHANGHAI DINGYA PHARMACEUTICAL CHEMICALS CO LTD (CN)
International Classes:
C07D207/34
Domestic Patent References:
| WO2010098286A1 | 2010-09-02 |
Foreign References:
| CN105164105A | 2015-12-16 | |||
| CN112707854A | 2021-04-27 | |||
| CN105473552A | 2016-04-06 | |||
| CN102186817A | 2011-09-14 | |||
| EP1844020A1 | 2007-10-17 | |||
| CN101679243A | 2010-03-24 |
Other References:
LIU YUXI, DAI HONGXING, DU YUCHENG, DENG JIGUANG, ZHANG LEI, ZHAO ZHENXUAN, AU CHAK TONG: "Controlled preparation and high catalytic performance of three-dimensionally ordered macroporous LaMnO3 with nanovoid skeletons for the combustion of toluene", JOURNAL OF CATALYSIS, ACADEMIC PRESS, DULUTH, MN., US, vol. 287, 1 March 2012 (2012-03-01), US , pages 149 - 160, XP093045756, ISSN: 0021-9517, DOI: 10.1016/j.jcat.2011.12.015
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