83790-87-8Relevant articles and documents
Preparation method of amiodarone hydrochloride key intermediate
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Paragraph 0030-0031; 0033-0034; 0036-0037; 0039-0040; 0042, (2021/11/03)
The invention discloses a preparation method of an amiodarone hydrochloride key intermediate. The method comprises the following steps: reacting benzofuranone with p-methoxybenzoyl chloride and valeryl chloride, and heating and reacting the product under an acidic condition to obtain the amiodarone hydrochloride key intermediate. According to the method, the key intermediate of amiodarone hydrochloride is prepared through a two-step simple reaction, the reaction condition is mild, byproducts are few, and aftertreatment is easy; due to the fact that aluminum trichloride is not used, no solid waste is generated; and the method has the advantages of simple route operation, high yield and lower cost than the existing route, and is very suitable for industrial production.
Benzofuran compound and application thereof
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Paragraph 0053-0057; 0062-0063; 0106-0107, (2021/08/06)
The invention provides a benzofuran compound as shown in a formula (I) or pharmaceutically acceptable salt thereof, and application thereof. The compound can selectively inhibit activation of NLRP3 inflammasomes and inhibit maturation and secretion of inflammation activation signal molecules Caspase-1 and P20 and inflammatory cytokines IL-1beta, has a good prevention and treatment effect on NLRP3 inflammasome related diseases, and particularly has a remarkable prevention and treatment effect on peritonitis and gouty arthritis. Therefore, the compound can be used for preparing drugs for treating NLRP3 inflammasome-related diseases, such as anti-inflammatory drugs or auxiliary anti-inflammatory drugs.
Lewis Acid-Catalyzed Synthesis of Benzofurans and 4,5,6,7-Tetrahydrobenzofurans from Acrolein Dimer and 1,3-Dicarbonyl Compounds
Huang, Wenbo,Xu, Jing,Liu, Changhui,Chen, Zhiyan,Gu, Yanlong
, p. 2941 - 2950 (2019/02/26)
2,3-Disubstituted benzofurans were synthesized from acrolein dimer and 1,3-dicarbonyl compounds by using N-bromosuccinimide as an oxidizing agent. The method was used to synthesize two commercial drug molecules, benzbromarone and amiodarone. The proposed mechanism of the reaction involves a N-bromosuccinimide (NBS)-assisted autotandem catalysis with Lewis acid catalyst. To proof the proposed mechanism, an intermediate was isolated successfully, which can be converted to 4,5,6,7-tetrahydrobenzofurans.