41964-07-2Relevant academic research and scientific papers
METHOD FOR PREPARING TOLIMIDONE ON LARGE SCALE
-
Paragraph 78-89, (2019/08/20)
The present disclosure relates to a method for preparing tolimidone on large scale with maintaining high purity and uniform particle size distribution, and more specifically, a method suitable for preparing tolimidone on industrially large scale by using
METHOD FOR PREPARING TOLIMIDONE ON LARGE SCALE
-
Paragraph 0074; 0075, (2018/04/13)
The present invention relates to a method for preparing tolimidone maintaining high purity and uniform particle distribution on a large scale. According to the present invention, high-purity tolimidone can be manufactured in a short time when compared to existing technologies while keeping the moisture content and grain size distribution constant by using a tetrabutylammonium bromide catalyst and ethanol recrystallization. Therefore, the method is suitable for industrial mass production.(AA) Before recrystallization(BB) After recrystallizationCOPYRIGHT KIPO 2018
Bronchodilator and Antiulcer Phenoxypyrimidinones
Lipinski, C. A.,Stam, J. G.,Pereira, J. N.,Ackerman, N. R.,Hess, H.-J.
, p. 1026 - 1031 (2007/10/02)
Series of 5-phenoxy-2(1H)-pyrimidinones, 5-phenoxy-4(3H)-pyrimidinones, and related compounds were prepared in a follow-up of a lead prepared as a potential cyclic nucleotide regulating agent.Compounds were evaluated for bronchodilator activity in histamine-challenged guinea pigs and for antiulcer activity in a cold-restraint, stressed rat ulcer model.Bronchodilator activity comparable to, or greater than, that of theophylline was found in both the 2(1H)- and 4(3H)-pyrimidinone series and was most prominent in analogues containing either an electron-withdrawing or -donating substituent in the para position of the phenoxy ring.Significant antiulcer activity was observed only in the 2(1H)-pyrimidinone series among three closely related analogues.One of these, 5-(m-methylphenoxy)-2(1H)-pyrimidinone (3), exhibited more potent antiulcer effects than the clinically useful antiulcer agent carbenoxolone, without demonstrating bronchodilator activity.
