141644-91-9Relevant articles and documents
Concise total synthesis of antiarrhythmic drug dronedarone via a conjugate addition followed intramolecular heck cyclization
Madhasu, Madhu,Doda, Sai Reddy,Begari, Prem Kumar,Dasari, Krishna Rao,Thalari, Gangadhar,Kadari, Sudhakar,Yadav, Jhillu Singh
, p. 1861 - 1866 (2021/07/09)
A concise, scalable, and an efficient total synthesis for dronedarone (2) was described using conjugate addition followed by intramolecular Heck cyclization. The other key reaction includes selective reduction of nitro functionality and addition of lithiated terminal alkyne to the aldehyde. The overall yield of this approach is 44% in six steps.
Benzofuran compound and application thereof
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, (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.
Preparation method of dronedarone hydrochloride key intermediate
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Paragraph 0022; 0031-0033, (2016/10/08)
The invention relates to a preparation method of a dronedarone hydrochloride key intermediate. The preparation method comprises following steps: 1) 2-butyl-benzofuran-5-ylamine hydrochloride and phthalic anhydride are subjected to reflux reaction under alkaline conditions so as to protect amino groups; and 2) 4-[3-(dibutyl amino) propoxy] benzoic acid is added into Eaton's reagent for stirring reaction, an intermediate 1 is added, temperature is controlled for reaction, a free amine is obtained via treatment, and the free amine and oxalic acid are subjected to salt forming reaction so as to obtain compound IV 5-amino-2-n-butyl-3-[4-(3-n-dibutyl aminopropoxy) benzoyl]benzofuran oxalate. The dronedarone hydrochloride key intermediate is prepared by taking 2-butyl-benzofuran-5-ylamine hydrochloride as the starting raw material; production of the dronedarone free amino is high in selectivity, and high in yield; fewer steps are needed; so that the preparation method is suitable for industrialized production.