107295-33-0Relevant articles and documents
Preparation method of important intermediate of levosimendan
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Paragraph 0059; 0075-0077; 0078; 0094-0096, (2020/03/29)
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.
PROCESS FOR PREPARING LEVOSIMENDAN AND INTERMEDIATES FOR USE IN THE PROCESS
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Page/Page column 12, (2011/02/24)
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.
Studies on agents with vasodilator and β-blocking activities. V. Synthesis and pharmacological activity of the optical isomers of TZC-5665
Seki, Toshimi,Kanada, Arihiro,Nakao, Tomio,Shiraiwa, Masahumi,Asano, Hajime,Miyazawa, Katuhiko,Ishimori, Tsutomu,Minami, Nobuyoshi,Shibata, Kenyu,Yasuda, Kikuo
, p. 84 - 96 (2007/10/03)
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).
