1044870-39-4Relevant articles and documents
Method for preparing apabetalone, intermediates and preparation method of intermediates
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Paragraph 0085-0092, (2020/05/30)
The invention provides a preparation method of apabetalone. The preparation method comprises the step of reacting a first intermediate, namely 2-bromo-4,6-dimethoxybenzoic acid with a second intermediate, namely 4-(2-hydroxyethoxy)-3,5-dimethylbenzamidine hydrochloride in an alkali-containing organic solvent under the action of a catalyst so as to obtain apabetalone. According to the invention, total yield is 33.4% or above, raw materials are easy to obtain, process is simple, reaction conditions are mild, post-treatment method is simple, the yield of each step and the total yield are high, and cost can be reduced. Apabetalone is a medicine for treating cardiovascular diseases such as atherosclerosis and the like, and has good application prospects. The invention also provides the intermediate 4-(2-hydroxyethoxy)-3,5-dimethylbenzamidine hydrochloride for synthesizing apabetalone and a preparation method thereof, and a preparation method of the compound 2-bromo-4,6-dimethoxybenzoic acid.
Design, synthesis and biological evaluation of hypolipidemic compounds based on BRD4 inhibitor RVX-208
Yu, Ping,Liu, Wenjing,Ren, Jinghui,Wang, Yingying,Ning, Yao,Huang, Mingqi,Hu,Wei, Lili,Ji, Min,Cai, Jin
, p. 2168 - 2172 (2019/07/03)
Bromodomain-containing protein 4 (BRD4) is a new therapeutic target for the treatment of diseases including cardiovascular diseases, cancer, inflammation and central nervous system (CNS) disorders. In this study, we introduced the pharmacophore of fibrates to a BRD4 inhibitor, RVX-208, to design dual-active hypolipidemic compounds, and found that some of new analogues showed favorable hypolipidemic activities. Synthetic accessibility towards this class of compounds optimized RVX-208 as well as would supply more thoughts on hypolipidemic drugs.
Based on BRD4 inhibitor RVX - 208 of the derivative and its preparation method and application (by machine translation)
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Paragraph 0041, (2018/09/21)
The invention discloses a method based on BRD4 inhibitor RVX - 208 of the derivative and its preparation method and application. Derivatives of the structure shown in formula I. The preparation method comprises: type 8 compound of formula 9 compound reaction, [...] 10 compound; type 10 compounds with malonic acid, d di-acid or fifth heavenly stem II acid after the reaction, with vinyl carbonate, 2 - halo of isobutyric acid or 4 - halo [...] butyric acid reaction; or, the type 10 compound directly with ethylene carbonate, 2 - halo of isobutyric acid or 4 - halo [...] butyric acid reaction. The invention also provides its application. The present invention provides based on BRD4 inhibitor RVX - 208 of the derivatives, can improve the activity or at the same time reducing cholesterol lowering cholesterol and triglyceride levels. (by machine translation)