Preparation method of Sugammadex sodium and intermediate thereof

Abstract

The present invention provides a preparation method of Sugammadex sodium and an intermediate thereof. The method comprises a bromination reaction of a compound of a formula (I) with a brominating reagent, wherein the brominating agent is selected from pyridinium tribromide. The method has the advantages of simple process, high yield, high purity and low pollution, and is suitable for industrial production.

Description

technical field [0001] The invention relates to a preparation method of sugammadex sodium and an intermediate thereof. Background technique [0002] Sugammadex sodium is the world's first selective antagonist of aminosteroid muscle relaxants developed by Merck & Co. First launched in Sweden in 2008, it is used to reverse muscle relaxation symptoms caused by rocuronium bromide or vecuronium bromide. On December 15, 2015, it was approved by the US FDA for marketing, and the trade name was Bridion (Bridion). [0003] Sugammadex sodium is a synthetic γ-cyclodextrin derivative, molecular formula: C 72 h 104 o 48 S 8 Na 8 , relative molecular mass: 2178.006. Its chemical structure is that 8 glucose molecules are connected end-to-end in the D-(+)-glucopyranose chair conformation to form a ring through α-1,4-glycosidic bonds, and the natural γ-ring is replaced by carboxyethyl sulfide group The hydroxyl group on the 6th carbon of each glucose molecule in dextrin deepens the i...

AI Technical Summary

Problems solved by technology

However, both the reaction and post-treatment of bromine are very cumbersome and dangerous in industry, so the process needs to be optimized and improved.

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