- Carbene-catalyzed enantioselective annulation of dinucleophilic hydrazones and bromoenals for access to aryl-dihydropyridazinones and related drugs
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4,5-Dihydropyridazinones bearing an aryl substituent at the C6-position are important motifs in drug molecules. Herein, we developed an efficient protocol to access aryl-dihydropyridazinone moleculesviacarbene-catalyzed asymmetric annulation between dinuc
- Chi, Yonggui Robin,Li, Xiangyang,Maiti, Rakesh,Mondal, Bivas,Tian, Weiyi,Xu, Jun,Yan, Jia-Lei,Yang, Xing
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Read Online
- Preparation method of important intermediate of levosimendan
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The invention belongs to the field, of synthesis of intermediates and relates to (R)- 6 - (4 -aminophenyl) - 5 - methyl - 444455-dihydropyridazine - 3333337. acetamide N - (4 - obtained by hydrolyzing)-methylpropionyl, phenyl, acetamide, in N - (4 - (3 - (-propionyl phenyl) - 2 - acetamide as starting material) and then chemical resolution.) yields high-purity,methylpropionyl (R)- N - (4 - (3 - (phenyl) - 2 - acetamide.). The present invention is very suitable for industrial production) by chemically resolving the high yield; dimethylamino,methylpropionyl-methaneanoyl-benzenesulfonamido (R)- N - (4 - (3 - phenylacetamido) obtained by hydrolyzing the intermediates with formaldehyde) dimethylamine. yields a high yield, yields a high yield of intermediate. The present invention relates to a, process for, producing high-chiral purified p-methyl propionylphenyl phenylacetonitrile.
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Paragraph 0059; 0075-0077; 0078; 0094-0096
(2020/03/29)
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- DIHYDROPYRIDAZINONES SUBSTITUTED WITH PHENYLUREAS
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Compounds of formula (I) which are nicotinamide phosphoribosyltransferase (NAMPT) inhibitors and their use for the treatment of hyperproloferative diseases and/or disorders responsive to induction of cell death.
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Page/Page column 221; 222
(2018/05/27)
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- PROCESS FOR PREPARING LEVOSIMENDAN AND INTERMEDIATES FOR USE IN THE PROCESS
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In an embodiment, the present invention provides a process for preparing (-)-6-(4- aminophenyl)-5-methylpyridazin-3-(2H)-one, which process comprises: a) reacting racemic 6-(4-aminophenyl)-4,5-dihydro-5-methyl-3-(2H)-pyridazinone of formula (Il) with a chiral tartaric acid derivative to obtain a diastereomeric salt of (-)-6-(4- aminophenyl)-4,5-dihydro-5-methyl-3-(2H)-pyridazinone and the chiral tartaric acid derivative; and b) reacting the diastereomeric salt with a base to obtain (-)-6-(4- aminophenyl)-4,5-dihydro-5-methyl-3-(2H)-pyridazinone. The (-)-6-(4-aminophenyl)-4,5- dihydro-5-methyl-3-(2H)-pyridazinone may be used to prepare levosimendan.
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Page/Page column 11
(2011/02/24)
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- Synthesis and anti-congestive heart failure activity of novel levosimendan analogues
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A series of levosimendan analogues were designed and synthesized, employing the Friedel-Crafts reaction, hydrolysis, and cyclization from the key intermediate compound R(-)-6-(4-aminophenyl)-5-methyl-4, 5-dihydro-3(2H)- pyridazinone, which was obtained from the starting material, acetanilide. These compounds, except 1b, exhibited potent anti-congestive heart failure activities, especially the compounds 1e and 1k, which showed more effective action than levosimendan. Springer Science+Business Media, LLC 2010.
- Wang, Lisheng,Zhou, Hongxiang,Yang, Bin,Chen, Zhigang,Yang, Hua
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p. 287 - 292
(2012/06/05)
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- Studies on agents with vasodilator and β-blocking activities. V. Synthesis and pharmacological activity of the optical isomers of TZC-5665
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Synthesis of the four optical isomers of TZC-5665 (1), a candidate for the treatment of congestive heart failure, was achieved by the reaction of chiral diaminopyridazinone (2) with chiral glycidyl ether (3). The hypotensive and β-blocking activities of 1 and its optical isomers were examined when given intravenously into anesthetized rats. Furthermore these compounds were evaluated for inhibitory activity on cAMP phosphodiesterase III. Among the four optical isomers, R(A),S(B)-one (1c) possessed the essential activities of TZC-5665 (1).
- Seki, Toshimi,Kanada, Arihiro,Nakao, Tomio,Shiraiwa, Masahumi,Asano, Hajime,Miyazawa, Katuhiko,Ishimori, Tsutomu,Minami, Nobuyoshi,Shibata, Kenyu,Yasuda, Kikuo
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