1545025-44-2Relevant articles and documents
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.
Synthesis technology of cardiovascular medicine Apabetalone
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Paragraph 0034; 0043; 0046; 0051; 0052; 0061, (2019/01/08)
The invention discloses a synthesis technology of a cardiovascular medicine Apabetalone, and relates to the technical field of organic synthesis of medicines. The synthesis technology comprises the following steps: with 3,5-dimethoxyaniline as a raw material, firstly performing a condensation reaction on the 3,5-dimethoxyaniline, hydroxylamine sulfate and chloral hydrate to obtain N-(2,4-dimethoxyphenyl)-2-(oximido)acetamide, then performing a cyclization reaction to obtain 5,6-dimethoxy isatin under the effect of concentrated sulfuric acid, then performing an oxidation reaction on the 5,6-dimethoxy isatin and ammonia water or ammonia gas to obtain 2-amino-4,6-dimethoxybenzonitrile in the presence of divalent copper and an oxidant, finally performing a condensation reaction on the 2-amino-4,6-dimethoxybenzonitrile and 4-(2-hydroxyethoxy)-3,5-dimethylbenzaldehyde in an organic solvent under the effect of an alkaline substance to obtain the Apabetalone. Compared with the synthesis technology recorded in the existing literature, the synthesis technology provided by the invention has the advantages as follows: the raw material is cheap and easy to obtain, a reaction condition is mild,high-temperature and high-pressure conditions are not required, the posttreatment operation is simple, a synthesis route is short, and industrial production is easy.
Based on BRD4 inhibitor RVX - 208 of the derivative and its preparation method and application (by machine translation)
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, (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)
PROCESSES FOR THE SYNTHESIS OF 2-AMINO-4,6-DIMETHOXYBENZAMIDE AND OTHER BENZAMIDE COMPOUNDS
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Paragraph 00163-00164, (2014/05/07)
This invention provides a method for the synthesis of a 2-amino-4,6-dimethoxybenzamide and other benzamides of Compound I: wherein R1, R2, R3, and R4 each independently represent a hydrogen, a C1-C6 alkyl, or a C1-C6 alkoxy; and wherein R6 and R7 each independently represent a hydrogen, a C1-C6 alkyl, a protecting group, or a directing group.
COMPOUNDS USEFUL IN THE SYNTHESIS OF BENZAMIDE COMPOUNDS
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, (2014/05/07)
Compounds that are useful in the synthesis of 2-amino-4,6-dimethoxybenzamide derivatives and other benzamide compounds.