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Preparation method of cardiovascular drug ketanserin tartrate

A technology of tartaric acid and ketanserin is applied in the directions of carboxylate preparation, organic chemistry and the like, and achieves the effects of high yield, simple process synthesis steps and improved bioavailability

Inactive Publication Date: 2019-06-04
辽宁博美医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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But the preparation method of ketanserin tartaric acid has not yet reported

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  • Preparation method of cardiovascular drug ketanserin tartrate
  • Preparation method of cardiovascular drug ketanserin tartrate

Examples

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Effect test

Embodiment example 1

[0016] In the 2000ml four-neck bottle equipped with mechanical stirring, reflux condenser and thermometer, add 10g ketanserin, 10g tartaric acid and 1000ml absolute ethanol, under stirring, be heated to 78 ℃, reaction time 8 hours. Cool and crystallize. A white solid was obtained by suction filtration, and dried to a constant weight of 13 g of white crystalline powder, with a calculated yield of 81%. mp: 187-189°C (dec.), the content reaches 99.1%.

Embodiment example 2

[0018] In the 1000ml four-neck bottle equipped with mechanical stirring, reflux condenser and thermometer, add 10g ketanserin, 10g tartaric acid and 400ml 95% ethanol; Under stirring, be heated to 80 ℃, reaction time 8 hours. Cool and crystallize. A white solid was obtained by suction filtration, and dried to a constant weight of 12.8 g of white crystalline powder, with a calculated yield of 80%. mp: 187-189°C (dec.), the content reaches 99.2%.

Embodiment example 3

[0020] In the 1000ml four-neck bottle equipped with mechanical stirring, reflux condenser and thermometer, add 10g ketanserin, 10g tartaric acid and 350ml 85% ethanol; Under stirring, be heated to 85 ℃, reaction time 6 hours. Cool and crystallize. A white solid was obtained by suction filtration, and dried to a constant weight of 12.0 g of white crystalline powder, with a calculated yield of 75%. mp: 187-189°C (dec.), the content reaches 99.3%.

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Abstract

The invention belongs to the field of drug synthesis, and provides a ketanserin tartrate preparation method, wherein ketanserin and DL-tartaric acid are used as raw materials, ethanol is used as a solvent, heating dissolving is performed, and the target product is directly obtained through crystallization. According to the present invention, with the method, the total yield can reach 80%, and theproduct purity exceeds 99.0%; and the method has advantages of simple process synthesis steps, substantially reduced production cost and low environment pollution, and substantially alleviates the environmental problem caused by the production of ketanserin tartrate.

Description

technical field [0001] The invention belongs to the field of drug synthesis, and in particular relates to a preparation method of cardiovascular drug ketoserin tartaric acid. Background technique [0002] Ketanserin (ketanserin), its chemical structure is pyridine derivatives. It can selectively block 5-HT2A receptors, without partial agonist effect; at the same time, it has weak blocking effect on α-receptors. As a new antihypertensive drug, ketanserin is mainly used in the treatment of cardiovascular diseases such as hypertension. In recent years, a large number of studies have made new developments in the clinical application of ketanserin. For example, the clinical experimental observation of 44 patients with stable angina pectoris caused by single vessel blockage by Kyriakides et al. showed that during coronary balloon angioplasty, intracoronary injection of ketanserin can significantly increase the number of coronary artery collaterals. Reduced blood flow occurs in ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/06C07C51/41C07C59/255
Inventor 周小明赵鸿伟王艳鲁执佳金建
Owner 辽宁博美医药科技有限公司
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