62827-49-0Relevant academic research and scientific papers
Method for preparing apabetalone, intermediates and preparation method of intermediates
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Paragraph 0067-0072, (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.
A New Secondary Metabolite from Alternaria Alternata: Structure Elucidation and Total Synthesis of Altenuic Acid IV
Kohler, Dominik,Podlech, Joachim
, p. 1748 - 1753 (2019/02/20)
A putative intermediate in the biosynthesis of altenuic acids I–III was isolated from Alternaria alternata in the 1950ies and a sample survived over the decades. This resorcylic lactone named altenuic acid IV is a composite of a resorcylic and a muconic a
Design and Synthesis of Metabolically Stable tRNA Synthetase Inhibitors Derived from Cladosporin
Rusch, Marion,Thevenon, Arnaud,Hoepfner, Dominic,Aust, Thomas,Studer, Christian,Patoor, Maude,Rollin, Patrick,Livendahl, Madeleine,Ranieri, Beatrice,Schmitt, Esther,Spanka, Carsten,Gademann, Karl,Bouchez, Laure C.
, p. 644 - 649 (2019/02/13)
Selective and specific inhibitors of Plasmodium falciparum lysyl-tRNA synthetase represent promising therapeutic antimalarial avenues. Cladosporin was identified as a potent P. falciparum lysyl-tRNA synthetase inhibitor, with an activity against parasite
Preparation method for Apabetalone
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Paragraph 0053; 0054, (2018/07/30)
The invention relates to a preparation method for Apabetalone, and particularly discloses a synthesis method for Apabetalone. The preparation method comprises the following steps: (1) a first intermediate, i.e., 2-bromo-4,6-dimethoxy benzamide, is prepared; (2) a second intermediate, i.e., 4-{2-[(t-butyldimethylsilicon)oxy]ethyoxyl}-3,5-dimethyl benzaldehyde, is prepared; (3) the first intermediate and the second intermediate are sealed under the conditions of cuprous bromide, cesium carbonate, L-proline and ammonia hydroxide to react, so that Apabetalone is obtained. The preparation method disclosed by the invention is simple, and yield is high.
Total Synthesis of the Resorcyclic Acid Lactone Spiroketal Citreoviranol
Quach, Rachelle,Furkert, Daniel. P.,Brimble, Margaret A.
, p. 8343 - 8350 (2016/09/28)
The first total synthesis of resorcyclic acid lactone spiroketal citreoviranol (1) is described. The synthesis was completed in nine steps and via Sonogashira cross-coupling, gold-catalyzed cyclization, and an unusual base-induced ketalization. The relati
