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Synthesis process of Sevelamer

A technique for the synthesis of Sevelamer hydrochloride, which is applied in the field of drug synthesis, can solve the problems of long reaction time and a large amount of organic solvents, and achieve the effects of shortened reaction time, simple operation, and strong phosphorus adsorption capacity

Active Publication Date: 2012-09-19
CHENGDA PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The reaction time required for this process is long, and many times of filtration and washing are required during the operation, and a large amount of organic solvents are required. Among the series of products, the highest phosphorus adsorption capacity is 3.1mmol / g

Method used

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  • Synthesis process of Sevelamer
  • Synthesis process of Sevelamer
  • Synthesis process of Sevelamer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1: the synthesis of Sevelamer Hydrochloride

[0027] In a 500mL flask, add 46.2g (0.374mol) polyallylamine hydrochloride, dissolve in 108.0mL deionized water, add sodium hydroxide to adjust pH=10-11, add dropwise 11.0g (0.042mol) 1-chloro The toluene solution of generation-3-p-toluenesulfonyl-2-propanol was reacted at 70-75°C for 4 hours. After the reaction is complete, add hydrochloric acid to adjust the pH=1-2, and filter to obtain the crude product of sevelamer hydrochloride. Disperse the crude product of Sevelamer Hydrochloride in 300.0 mL of deionized water, add sodium hydroxide to adjust the pH=10.0-11.0, filter, wash with deionized water, and dry the white solid at 70°C for 8 hours in vacuum, then pulverize to obtain the product Sevelamer hydrochloride is 38.8g, the phosphorus adsorption value is 5.5mmol / g, and the chloride ion content is 16.5%.

Embodiment 2

[0028] Embodiment 2: the synthesis of carbonic acid sevelamer

[0029] In a 500mL flask, add 150.0g (0.404mol, weight concentration: 30%) polyallylamine hydrochloride aqueous solution, add sodium hydroxide to adjust pH=10-11, add dropwise 13.0g (0.042mol) 1-bromo Substitute-3-p-toluenesulfonyl-2-propanol in acetonitrile solution, heat up at 70-75°C for 4 hours. After the reaction is complete, add hydrochloric acid to adjust the pH=1-2, and filter to obtain the crude product of sevelamer hydrochloride. Disperse the crude product of sevelamer hydrochloride in 300.0mL deionized water, add sodium carbonate to adjust the pH=8.5-9.5, filter, wash with deionized water, and dry the white solid at 70°C for 8 hours in vacuum, and then pulverize it to obtain the product carbonic acid Sevelamer 36.4g, phosphorus adsorption value 5.4mmol / g.

Embodiment 3

[0030] Embodiment 3: the synthesis of carbonic acid sevelamer

[0031] In a 500mL flask, add 46.2g (0.374mol) polyallylamine hydrochloride, dissolve in 108.0mL deionized water, add sodium hydroxide to adjust pH=10-11, add dropwise 7.9g (0.042mol) 1-chloro Substitute-3-methylsulfonyl-2-propanol in toluene solution, heat up at 70-75°C for 4 hours. After the reaction is complete, add hydrochloric acid to adjust the pH=1-2, and filter to obtain the crude product of sevelamer hydrochloride. Disperse the crude product of sevelamer hydrochloride in 300.0 mL of deionized water, add sodium hydroxide to adjust the pH=12.0-12.5, pass in carbon dioxide gas to saturation, filter, wash with deionized water, and dry the white solid at 70°C for 8 hours in vacuum , and then pulverized to obtain 40.5 g of the product sevelamer carbonate, with a phosphorus adsorption value of 5.0 mmol / g.

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Abstract

The invention discloses a synthesis process of Sevelamer, particularly provides a new method for synthesising Sevelamer, which is suitable for industrial production, low in cost and simple in operation, wherein the method can be used for producing the hydrochloride or carbonate of Sevelamer, and belongs to the field of medicine synthesis. According to the invention, 1-halo-3-sulfonyloxyl-2-propyl alcohol is used as a cross-linking agent, and reactes with polyene propylamine hydrochloride in an alkaline condition to generate cross-linked polyene propylamine, and the hydrochloride or carbonate of Sevelamer is obtained by process steps such as acidification and salification. Compared with other synthesis methods, the process flow is simple and convenient to operate, the reaction time is shorten by more than 70%, and the phosphorus adsorption capacity of the product is strong and up to 5.0-6..0 mmol / g.

Description

technical field [0001] The invention belongs to the field of drug synthesis and relates to a method for synthesizing Sevelamer, which can be used to treat hyperphosphatemia. Background technique [0002] Hyperphosphatemia is a condition that often occurs in patients with renal dysfunction, hypothyroidism, acute acromegaly, or phosphate drug overdose and is usually treated with food therapy or oral phosphate adsorbent drug therapy However, it is generally considered that food therapy is less effective and the use of phosphorus adsorbents is essential. In recent years, studies have found that compounds containing polyallylamine structures have good phosphorus adsorption capacity (such as: US patent 5496545, 20040191212, Chinese patent 95193521.6, etc.), and cross-linked polyallylamine drugs are even more effective. Due to its good clinical performance, Sevelamer has been approved for marketing for the treatment of hyperphosphatemia. The structural formula of Sevelamer is as ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08F126/02C08F8/44C08J3/24C08K5/42A61P3/12
Inventor 彭智勇李继超文春林葛建利
Owner CHENGDA PHARM CO LTD
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