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Preparation method for high-purity rocuronium bromide

A high-purity technology of rocuronium bromide, which is applied in the field of medicine, can solve problems such as easy degradation, difficult drying of solvates, and moisture absorption, and achieve the effects of reducing impurity levels, improving drug safety, and simple production technology and operation

Pending Publication Date: 2020-05-01
CHENGDU SINO STRONG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0015] Based on the above problems, the present invention provides a preparation method of high-purity rocuronium bromide, which solves the problems of easy degradation, moisture absorption, easy formation of solvates and difficult drying of rocuronium bromide in the purification process, and can improve the production efficiency of rocuronium bromide. The purity of curonium bromide is more than 99.95%

Method used

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  • Preparation method for high-purity rocuronium bromide
  • Preparation method for high-purity rocuronium bromide
  • Preparation method for high-purity rocuronium bromide

Examples

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Embodiment 1

[0055] Embodiment 1: the preparation of low-purity rocuronium bromide

[0056] Add 500g of dichloromethane to a 1000ml flask, add (2β,3α,5α,16β,17β)-17-acetoxy-3-hydroxyl-2-(4-morpholinyl)-16-(1-pyrrolidine Base) androstane 100g, stir until the solid is completely dissolved, add 100g sodium carbonate and 100g 3-bromopropene, and react at 20-30°C. After the reaction was completed, the inorganic salt was removed by filtration, the filter cake was washed with dichloromethane, and the filtrate was dropped into 4000 g of ether, stirred and dispersed, filtered, washed, and dried under reduced pressure at 45 to 50° C. to obtain 119 g of rocuronium bromide, with a yield of 95.2%. 98.5% purity. Low-purity rocuronium bromide HPLC chromatogram such as figure 1 .

Embodiment 2

[0057] Embodiment 2: the preparation of high-purity rocuronium bromide

[0058] Add 10 g of low-purity rocuronium bromide prepared in Example 1 to 50 g of acetone, 1 g of methanol, and 2.5 g of ether, stir at 20 to 30 ° C to dissolve the solid, stir and crystallize at -20 to -15 ° C for 48 hours, filter, Dry under reduced pressure at 10-20°C to obtain 6.78g of high-purity rocuronium bromide, with a yield of 67.8%, the largest single impurity 0.015%, and the total impurity 0.040%.

[0059] After testing, its HPLC spectrum is as follows figure 2 shown.

Embodiment 3

[0060] Embodiment 3: the preparation of high-purity rocuronium bromide

[0061] Add 11 g of low-purity rocuronium bromide prepared in Example 1 to 45 g of butanone, 1.2 g of methanol and 2.0 g of methyl tert-butyl ether, stir at 20 to 30°C to dissolve the solid, and stir at -10 to -5°C Crystallize for 30 hours, filter, and dry under reduced pressure at 10-20°C to obtain 5.76 g of high-purity rocuronium bromide, with a yield of 52.3%, the largest single impurity 0.014%, and total impurities 0.034%.

[0062] After detection, its HPLC collection of illustrative plates and figure 2 Basically the same.

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Abstract

The invention discloses a preparation method for high-purity rocuronium bromide. The high-purity rocuronium bromide is prepared by recrystallizing low-purity rocuronium bromide in an organic solvent.The technical process for preparing the rocuronium bromide is simple to operate; the total content of impurities in a prepared product does not exceed 0.05%; and the quality condition of the preparedproduct is far superior to the quality condition of a product purified by using a conventional method. The high-purity rocuronium bromide provided by the invention has significant advantages in stability, is not easy to degrade, and is more beneficial to production, storage and transportation.

Description

technical field [0001] The invention relates to the field of medicine, in particular to the preparation of rocuronium bromide. Background technique [0002] Muscle relaxants are necessary adjuvant drugs for anesthesia in surgical operations, and are used in large amounts. At present, the common ones are rocuronium bromide, vecuronium bromide, succinylcholine, and atracurium bromide. Rocuronium Bromide (Chinese name: Rocuronium bromide), chemical name 1-[(2β,3α,5α,16β,17β)-17-(acetyloxy)-3-hydroxy-2-(4-morpholinyl) Androstan-16-yl]-1-(2-propenyl)pyrrolidine bromide is a steroidal non-depolarizing muscle relaxant developed by Organon in the Netherlands. Because rocuronium has the fastest onset of action and no side effects such as releasing histamine, it becomes the most promising drug among similar drugs. Since the development of Organon in the Netherlands, it has been marketed in more than 40 countries and regions including the Netherlands, Belgium, Germany, the United Sta...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J43/00
CPCC07J43/003
Inventor 高建王成刚匡建明李有章刘力超伍伟
Owner CHENGDU SINO STRONG PHARMA
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