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Racemization method of 6-4-(4-amino pheny)-4, 5-dihydro-5-methyl-3-(2H)-pyridazinone

A kind of technology of aminophenyl, pyridazinone dextromer, applied in 6--4 field, can solve problems such as waste

Inactive Publication Date: 2005-05-18
GUANGXI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, in the preparation of levosimendan and pimobendan, only 6-(4-aminophenyl)-4,5-dihydro-5-methyl-3-(2H)-pyridazinone is required. L-isomer, the reaction process produces a large amount of D-isomer, if it is poured out, it will be a great waste
In order to reduce waste and reduce costs, many pharmaceutical chemists have made many efforts to solve this problem, but it has been unsuccessful

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Dissolve 10g of 6-(4-aminophenyl)-4,5-dihydro-5-methyl-3-(2H)-pyridazinone dextrorotatory 5g NaOH in 100ml of methanol, reflux for 24 hours, evaporate to dryness, and wash with tap water Wash with water to pH 7-8, and dry in an oven at 70°C for 5 hours to obtain 7.8 g of solid. [α] D 25 =0

Embodiment 2

[0017] Dissolve 10g of 6-(4-aminophenyl)-4,5-dihydro-5-methyl-3-(2H)-pyridazinone dextrorotatory 5g NaOH in 100ml ethanol, reflux for 24h, evaporate to dryness, and distilled water Wash with water to pH 7-8, and dry in an oven at 80°C for 4 hours to obtain 8 g of solid. [α] D 25 =0

Embodiment 3

[0019] Dissolve 10g of 6-(4-aminophenyl)-4,5-dihydro-5-methyl-3-(2H)-pyridazinone dextrorotate, 5g of NaOH in 100ml of 1,4-dioxane, and reflux for 24h Afterwards, it was washed with tap water until the pH was 7-8, and dried in an oven at 90° C. for 3 hours to obtain 8.1 g of solid. [α] D 25 =0

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Abstract

The present invention relates to the processing method of 6-(4-amino phenyl)-4, 5-dihydro-5-methyl-3-(2H)-pyridazinone as the intermediate material for levosimendan and pimobendan as cardiac and cerebral vascular diseases medicine. The processing includes the first mixing of 6-(4-amino phenyl)-4, 5-dihydro-5-methyl-3-(2H)-pyridazinone dextroisomer with alkali or acid in 50 %, dissolving with solvent and reflux, evaporation to dry, water washing, and drying to obtain product. The said method can raise material utilization rate and lower product cost, and through four times one racemization and five times of resolution, the accumulated yield may reach 30-40 %, with the single time resolution yield being 8-12 %.

Description

technical field [0001] The invention relates to an intermediate raw material 6-(4-aminophenyl)-4,5-dihydro-5-methyl-3-(2H)- Process for the treatment of pyridazinones, in particular for the racemization of 6-(4-aminophenyl)-4,5-dihydro-5-methyl-3-(2H)-pyridazinone. Background technique [0002] Acute heart failure is a disease related to hemodynamic changes, and the treatment should start from the hemodynamic point of view. Chronic heart failure is related to neurohormones, and neurohormones need to be adjusted during treatment. The current treatment methods for acute heart failure mainly include intravenous diuretics, vasodilators and myocardial contractility enhancers. Medical experts believe that the treatment of acute heart failure should be the same as that of chronic heart failure, that is, to improve symptoms and reduce the risk of death or severe heart failure. Long-term use of myocardial contractility enhancers is harmful, but short-term use is beneficial. The ne...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D237/14
Inventor 王立升李子同周永红李伟光李艳琳刘雄民
Owner GUANGXI UNIV
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