Title:
SYNTHESIS METHOD FOR FINERENONE AND INTERMEDIATE THEREOF
Document Type and Number:
WIPO Patent Application WO/2023/109968
Kind Code:
A2
Abstract:
The invention provides a new synthesis method for a finerenone intermediate. The method comprises: (1) in the presence of an acid and in an inert solvent or under solvent-free conditions, reacting diethyl malonate, 4-cyano-2-methoxybenzaldehyde and 4-amino-5-methyl-2-hydroxypyridine to prepare compound 1; (2) subjecting compound 1 obtained in step (1) and triethyl orthoformate to an alkylation reaction in an inert solvent or under solvent-free conditions under the catalysis of an acid to obtain compound 2; (3) reducing compound 2 obtained in step (2) by using a reducing agent to obtain compound 3; and (4) in the presence of a catalyst, subjecting compound 3 and alcohol to chemical resolution to prepare chiral compound 4. The reaction formula is shown as follows: . By means of the technical solution of the present invention, the use of a chiral column resolution method is avoided, so that the cost is reduced; and by means of the chemical resolution, the loss of raw materials is reduced, the post-treatment is simple, and industrial large-scale production is facilitated.
Inventors:
RUAN SHIWEN (CN)
ZHANG WEI (CN)
YAN GONGCHAO (CN)
ZHANG XINXIN (CN)
ZHANG WEI (CN)
YAN GONGCHAO (CN)
ZHANG XINXIN (CN)
Application Number:
PCT/CN2022/139823
Publication Date:
June 22, 2023
Filing Date:
December 18, 2022
Export Citation:
Assignee:
SHANGHAI DINGYA PHARMACEUTICAL CHEMICALS CO LTD (CN)
International Classes:
C07D471/04
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