803684-91-5

Upstream product

• 67305-24-2 5-methylisoxazole-4-carbonyl chloride 
• 636992-57-9 (E)-3-[3-amino-2-(4-cyanobenzoyl)benzo[b]furan-5-yl]but-2-enoic acid diethylamide 
• 42831-50-5 5-methyl-1,2-oxazole-4-carboxylic acid 
• 40530-18-5 5-bromo-2-hydroxybenzonitrile 
• 20099-89-2 4-Cyanophenacyl bromide 
• 636992-59-1 4-(3-amino-5-bromo-benzofuran-2-carbonyl)-benzonitrile 
• 1950-58-9 (E)-N,N-diethyl-2-butenamide 

Relevant academic research and scientific papers

BENZOFURAN COMPOUND AND MEDICINAL COMPOSITION CONTAINING THE SAME

The present invention relates to a benzofuran compound of the formula (I) wherein each symbol is as defined in the description, a pharmaceutically acceptable salt thereof and the like. The compound of the present invention has superior leukotriene inhibitory action, BLT2 competitive inhibitory action, BLT2 blocking action, action for the prophylaxis or treatment of allergy, action for the prophylaxis or treatment of asthma and action for the prophylaxis or treatment of inflammation, and is useful as an agent for the prophylaxis or treatment of diseases such as allergic disease, asthma, inflammation and the like, and other diseases.

Syntheses of 3-acetoacetylaminobenzo[b]furan derivatives having cysteinyl leukotriene 2 receptor antagonistic activity

Novel 3-acetoacetylaminobenzo[b]furan derivatives having a modified triene system at the 3-position were synthesized starting with 3-aminobenzo[b]furans. The enol isomers, 3-[(3-hydroxybul-2-enonyl)amino]benzo[b]furans (1), of the 3-acetoacetylaminobenzo[b]furans were obtained as stable isomers owing to formation of a hydrogen bonding between the enol hydroxyl group and the amidocarbonyl group. The planarity of the C-2 substituent through the C-3 side chain suggested the existence of a modified conjugational triene system in the enol compound. Cysteinyl leukotriene 1 and 2 receptor antagonistic activities for these compounds were evaluated. 2-(4-Cyanobenzoyl or ethoxycarbonyl)-3-[(2-cyano-3-hydroxybut-2-enonyl)amino]benzo[e]furans (15g, 15o, 15u) were moderately active.