16960-49-9Relevant articles and documents
Synthesis method of levosimendan drug intermediate p-acetaminophenylethylketone
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Paragraph 0015; 0016, (2016/11/21)
The invention relates to a synthesis method of a levosimendan drug intermediate p-acetaminophenylethylketone, which comprises the following steps: adding 430-460ml of cyclohexane into a 1.5L reaction vessel which is provided with a stirrer, a reflux condenser and a thermometer, cooling the solution to 6-9 DEG C, slowly adding 2.9-3.1 mol of stannous chloride, refluxing for 80-120 minutes, and adding 1.0 mol of acetanilide in batches within 2-3 hours; after finishing addition, continuing reacting for 60-90 minutes, and adding 110ml of propanamide under reflux conditions within 3-4 hours; and after finishing addition, continuing refluxing for 5 hours until the solution becomes dark, distilling to remove the cyclohexane, heating the solution to 85-90 DEG C, reacting for 3-4 hours, adding the reaction product into 2.3L of oxalic acid solution, controlling the stirring rate at 160-190 rpm, precipitating a solid, filtering, washing the solid with a salt solution, washing with triethylamine, dehydrating with a dehydrating agent, and recrystallizing in propionitrile to obtain the p-acetaminophenylethylketone.
Synthesis and anti-congestive heart failure activity of novel levosimendan analogues
Wang, Lisheng,Zhou, Hongxiang,Yang, Bin,Chen, Zhigang,Yang, Hua
experimental part, p. 287 - 292 (2012/06/05)
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.
NOVEL BENZIMIDAZOLEDIHYDROTHIADIAZINONE DERIVATIVES AS FRUCTOSE-1,6-BISPHOSPHATASE INHIBITORS, AND PHARMACEUTICAL COMPOSITIONS COMPRISING SAME
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Page/Page column 74, (2009/06/27)
The present invention relates to novel benzimidazole-dihydrothiadiazinone derivatives as fructose-1,6-bisphosphatase inhibitors, to processes for the preparation thereof and to the use thereof in therapy, especially for the treatment of diabetes.