- METHOD FOR PREPARING TOLIMIDONE ON LARGE SCALE
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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
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Paragraph 78-89
(2019/08/20)
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- METHOD FOR PREPARING TOLIMIDONE ON LARGE SCALE
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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
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Paragraph 0074; 0075
(2018/04/13)
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- Bronchodilator and Antiulcer Phenoxypyrimidinones
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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.
- Lipinski, C. A.,Stam, J. G.,Pereira, J. N.,Ackerman, N. R.,Hess, H.-J.
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p. 1026 - 1031
(2007/10/02)
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