Preparation method of pimobendan

A technology for the preparation of pimobendan and its preparation technology, which is applied in the field of preparation of pimobendan, and can solve problems such as being unsuitable for industrial scale-up production

Pending Publication Date: 2021-10-08
江苏君若药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] Based on the above-mentioned methods for the synthesis of pimobendan that have been publicly reported, the US4361563 patent, the synthetic route reported by Pu Riyang, the synthetic route reported by Wang Sisi,

Method used

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  • Preparation method of pimobendan
  • Preparation method of pimobendan
  • Preparation method of pimobendan

Examples

Experimental program
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Embodiment

[0023] Add compound formula I (100g, 325.6mmol) and Cs to the reaction bottle for preparing pimobendan 2 CO 3 (265.2g, 814mmol, 2.5eq), under the protection of nitrogen, Dioxane (5.0L) and DMF (2.0L) were added to the reaction system. After the addition, the system was stirred and degassed under vacuum at room temperature for 1 hour, and then p-methoxyphenylboronic acid pinacol ester (152.4g, 651.0mmol, 2.0eq) and PdCl were added to the reaction system under nitrogen protection. 2 (PPh 3 ) 2 (22.9 g, 32.6 mmol, 0.1 eq). After the addition, the system was replaced with nitrogen 3 times. The system was heated to 80-85°C for 12 hours, and then cooled down to room temperature naturally. After filtration, the filtrate was concentrated under reduced pressure to remove the organic solvent. Add DMF (2.0L) to the residue, slowly raise the temperature until the system dissolves, then slowly add H to the system while maintaining the temperature 2 O (3.0L), the system was stirred f...

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Abstract

The invention relates to a novel preparation process of pimobendan. Specifically, a Suzuki coupling reaction is carried out on a compound shown as a formula I (6-(2-bromo-1H-benzo[d]imidazol-6-yl)-5-methyl-4, 5-dihydropyridazin-3(2H)-one) and a compound shown as a formula II (p-methoxyphenylboronic acid or p-methoxyphenylboronic acid pinacol ester) under the action of a Pd catalyst, so that the preparation of the pimobendan is realized.

Description

technical field [0001] The present invention relates to the preparation of pimobendan. Background technique [0002] Pimobendan was developed by Boehringer Ingelheim of Germany and was first listed in Japan in 1994 as a cardiotonic drug with a vasodilator effect. It belongs to phosphodiesterase inhibitors and is mainly used clinically for the treatment of heart failure. . The compound is a cardiotonic dilator compound with calcium sensitization and type III phosphatase inhibitors, and its mechanism of action is different from that of traditional cardiotonic drugs. 2+ Sensitivity and inhibition of phosphodiesterase III (PDE III), is the first calcium sensitizer drug on the market. Studies have shown that the drug has a strong vasodilator effect and anti-platelet aggregation effect, almost no side effects, can also treat chronic heart insufficiency and angina, and can also prevent and treat arterial thrombosis. In addition, a large number of clinical trials have also shown ...

Claims

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Application Information

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IPC IPC(8): C07D403/04
CPCC07D403/04
Inventor 方显杰蔡泉
Owner 江苏君若药业有限公司
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