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Preparation method of mosapride citrate impurity

A technology for mosapride citrate and impurities, which is applied in the field of drug synthesis and achieves the effects of strong operability, mild reaction conditions and good reproducibility

Pending Publication Date: 2021-01-12
深圳市祥根生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

At present, the preparation method of this impurity has not been reported

Method used

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  • Preparation method of mosapride citrate impurity

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Effect test

Embodiment 1

[0021] Preparation of compound Ⅲ: compound Ⅰ (1.00g, 4.46mmol), 2-aminomethyl-4-(4-fluorobenzyl) morpholine (formula Ⅱ) (1.06 g, 4.90mmol) EDCI (1.24g, 8.47 mmol) and HOBT (1.08g, 8.03mmol) were dissolved in DMF (30ml), and triethylamine (0.65g, 6.47mmol) was slowly added dropwise at -20°C. React at room temperature for 3 hours. After the reaction, add water (10ml) to the reaction system, and a large amount of white solid precipitates out. Suction filtration, the filter cake is purified by column chromatography to obtain 1.68g of white solid compound III with a yield of 89%.

[0022] Preparation of Compound V: Compound IV (2.00 g, 7.63 mmol) was dissolved in dry dichloromethane, oxalyl chloride (1.76 g, 13.87 mmol) was slowly added dropwise at 0°C, and the temperature was raised to room temperature to continue the reaction for 1 h. The reaction solution was concentrated to dryness to obtain compound V, which was directly used in the next step without purification.

[0023] Pr...

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PUM

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Abstract

The invention discloses a preparation method of a mosapride citrate impurity, which comprises the following steps: by using 2-amino-4-chloro-5-ethoxybenzoic acid as a raw material, carrying out four steps of reaction to synthesize the mosapride citrate impurity. The method is reasonable in synthetic route design, mild in reaction condition and simple in post-treatment; the process is stable, the reproducibility is good, and the operability is high; and the purity of the mosapride impurity prepared by the method can reach 98% or above, a qualified impurity reference substance can be provided for quality control of mosapride, and the method has important application value.

Description

technical field [0001] The invention belongs to the field of drug synthesis, in particular to a method for preparing mosapride citrate impurities. Background technique [0002] Mosapride citrate is a selective 5-hydroxytryptamine 4 (5-HT4) receptor agonist, which can promote the release of acetylcholine, stimulate the gastrointestinal tract and play a prokinetic effect, thereby improving functional dyspepsia. Gastrointestinal symptoms, but does not affect gastric acid secretion. It has no affinity with dopamine D2 receptors, adrenaline α1 receptors, 5-HT1 and 5-HT2 receptors on the synaptic membrane of brain nerve cells, so it will not cause extrapyramidal syndrome and cardiovascular adverse reactions. Therefore, it is often used clinically for patients with functional dyspepsia with symptoms such as epigastric fullness, nausea, vomiting, acid reflux, and heartburn. It can also be used for reflux esophagitis, gastroparesis, and after partial gastrectomy. patients with dysp...

Claims

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Application Information

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IPC IPC(8): C07D265/30
CPCC07D265/30
Inventor 孙坤杰
Owner 深圳市祥根生物科技有限公司
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