Unlock instant, AI-driven research and patent intelligence for your innovation.

A kind of preparation method of sugammadex sodium

A technology of sugammadex sodium and sodium ions, which is applied in the field of preparation of sugammadex sodium, and can solve the problems of long reaction route and cumbersome operation

Active Publication Date: 2021-05-11
BRIGHTGENE BIO MEDICAL TECH (SUZHOU) CO LTD
View PDF11 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] The above method generally has the disadvantages of long reaction route and cumbersome operation.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • A kind of preparation method of sugammadex sodium

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] 2L three-neck flask, under nitrogen protection, add 1000ml of DMF and γ-cyclodextrin (100.0g 0.077mol), then add 3-mercaptopropionic acid (73.6g 0.694mol), cool down to -35°C, add trifluoromethane dropwise Sulfonic acid (98.4g 0.655mol), the temperature is controlled not to exceed -30°C, and the reaction is kept stirring for 3h. Add 5M aqueous sodium hydroxide solution dropwise to the reaction solution, adjust the pH to 9-10, heat up to 25°C and stir to react for 2 hours, suction filtration to obtain a solid, use DMF: water = 3:1 to beat for 2 hours, and filter to obtain smoother glucose Crude sodium product, yield: 70%, purity: 98%.

Embodiment 2

[0022] 2L three-neck flask, under nitrogen protection, add 1000ml of DMSO and γ-cyclodextrin (100.0g 0.077mol), then add 3-mercaptopropionic acid (73.6g 0.694mol), cool down to -35°C, add trifluoromethane dropwise Sulfonic acid (98.4g 0.655mol), the temperature is controlled not to exceed -30°C, and the reaction is kept stirring for 3h. 5M sodium methoxide aqueous solution was added dropwise to the reaction solution, adjusted to pH 9-10, the temperature was raised to 25°C and stirred for 2h, suction filtration to obtain a solid using DMF:water = 3:1, beating for 2h, and filtered to obtain sodium gluconate. Crude. Yield: 65%, Purity: 96%

Embodiment 3

[0024] 2L three-neck flask, under nitrogen protection, add 1000ml of formamide and γ-cyclodextrin (100.0g 0.077mol), then add 3-mercaptopropionic acid (73.6g 0.694mol), cool down to -35°C, add dropwise trifluoro Methanesulfonic acid (98.4g, 0.655mol), the temperature was controlled not to exceed -30°C, and the reaction was kept stirring for 3h. Add 5M aqueous sodium ethoxide solution dropwise to the reaction solution, adjust the pH to 9-10, heat up to 25°C and stir to react for 2 hours, suction filtration to obtain a solid, use DMF: water = 3:1 to beat for 2 hours, and filter to obtain sodium gluconate. Crude. Yield: 66%, Purity: 97%

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention discloses a preparation method of sugammadex sodium. The method is obtained by reacting γ-cyclodextrin with 3-mercaptopropionic acid and trifluoromethanesulfonic acid, and then using an alkali metal solution containing sodium ions to quench the reaction. Sugammadex Sodium. The present invention uses a one-step method to synthesize sugammadex sodium, reduces reaction steps, reduces costs, has high yield and purity, and is beneficial to industrial production. In addition, no halogen is used in the present invention, which reduces environmental pollution.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparation, in particular to the preparation of sugammadex sodium. Background technique [0002] Sugammadex sodium is a new type of selective muscle relaxant antagonist, which can selectively bind to amino carrier muscle relaxants and terminate their muscle relaxation effects. The drug is a modified γ-cyclodextrin with a cyclic molecular structure composed of 8 adjacent glucose molecules with a lipophilic inner cavity with an inner diameter optimal for accommodating amino carrier molecules such as rocuronium bromide. Eight negatively charged and hydrophilic carboxyl side chains project outward from the edge of the cyclodextrin molecule, and the acidic functional group (COO—) on the side chain increases the lipophilicity of the inner cavity of sugammadex and can interact with Roku. The positively charged nitrogen atoms of ammonium bromide form electrostatic bonds. At the same time, these groups rep...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): C08B37/16
Inventor 袁建栋黄仰青池建文葛亮
Owner BRIGHTGENE BIO MEDICAL TECH (SUZHOU) CO LTD