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Simple preparation method of acotiamide

The technology of acotiamide and acotiamide hydrochloride is applied in the field of simple and convenient preparation of acotiamide, can solve the problems such as not obtaining acotiamide crystals, and achieves an economical and environmentally friendly production process, simple operation and high yield. Effect

Inactive Publication Date: 2018-01-09
FUZHOU MINHAI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, since dichloromethane or chloroform is immiscible with water, the crystallization and layering are obvious after standing, and no crystallization of acotiamide has been obtained after repeated attempts.

Method used

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  • Simple preparation method of acotiamide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Add 100mL of water and 100mL of methanol into the reaction bottle, stir evenly, add 100.00g of acotiamide hydrochloride crude product, control the temperature at 10°C, add 14.75g of sodium bicarbonate in three equal parts; after adding sodium bicarbonate, continue to control the temperature at 10°C Stir for 3 hours; after stirring, filter and wash the filter cake with 100 mL of water; vacuum dry the wet powder, control the drying temperature at 45° C. and vacuum dry until the moisture content is ≤ 2.0%, to obtain 90.22 g of acotiamide dry powder, with a molar yield of 96.74%, HPLC The purity is 99.5%.

Embodiment 2

[0027] Add 200mL of water and 200mL of methanol into the reaction bottle, stir evenly, add 100.00g of acotiamide hydrochloride crude product, control the temperature at 15°C, add 15.52g of sodium bicarbonate in four equal parts; after adding the sodium bicarbonate, continue to control the temperature for 15 Stir at ℃ for 3.5 hours; after stirring, filter and wash the filter cake with 150mL of water; vacuum-dry the wet powder, control the drying temperature at 50°C and vacuum-dry until the moisture content is ≤2.0%, to obtain 89.91g of acotiamide dry powder, and the molar yield is 96.41%. HPLC purity 99.6%.

Embodiment 3

[0029] Add 300mL of water and 300mL of methanol into the reaction bottle, stir evenly, add 100.00g of acotiamide hydrochloride crude product, control the temperature at 20°C, add 16.30g of sodium bicarbonate in five equal parts; after adding the sodium bicarbonate, continue to control the temperature for 20 Stir at ℃ for 4 hours; complete the stirring, filter, and wash the filter cake with 200 mL of water; vacuum-dry the wet powder, control the drying temperature at 55 °C and vacuum-dry until the moisture content is ≤ 2.0%, to obtain 89.85 g of acotiamide dry powder, and the molar yield is 96.34%. HPLC purity 99.7%.

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Abstract

The invention discloses a simple preparation method of acotiamide. The preparation method comprises suspending a crude acotiamide hydrochloride product in a fatty alcohol and water solution, controlling the temperature in a range of 10-20 DEG C, adding sodium bicarbonate in several times, after the sodium bicarbonate is completely added, continuously controlling the temperature in a range of 10-20DEG C, performing stirring for 3-4 h, performing filtration, washing the obtained filtered cake with water, and performing vacuum drying to the obtained wet powder to obtain acotiamide. The preparation method is simple to operate, suitable for large-scale production and economic and eco-friendly in production process. The prepared acotiamide is high in yield and purity and is beneficial for further obtaining high-quality acotiamide hydrochloride.

Description

technical field [0001] The invention relates to a simple and convenient preparation method of acotiamide. Background technique [0002] Acotiamide hydrochloride hydrate, the chemical name is N-[2-(diisopropylamino)ethyl]-2-[(2-hydroxy-4,5-dimethoxybenzoyl) Amino]-1,3-thiazole-4-carboxylic acid amine hydrochloride trihydrate, jointly developed by Japan Astella Pharmaceuticals and Zeli Shinyaku Co., Ltd., was approved in Japan in June 2013 for the treatment of Functional dyspepsia (FD) has a good therapeutic effect on postprandial fullness, early satiety and upper abdominal pain caused by FD. It is the first drug in the world that has a definite curative effect on FD patients and is safe and guaranteed. Its chemical structure is: [0003] [0004] Since it was launched in Japan in 2013, acotiamide hydrochloride has received extensive attention from all walks of life around the world. FD is a relatively common disease in gastroenterology. Some people suffer from this dis...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D277/56
Inventor 张发香宁金洋陈娇娇
Owner FUZHOU MINHAI PHARMA
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