Method for preparation and semi-synthesis of galanthamine hydrobromide

Abstract

The invention relates to a method for the preparation and the semi-synthesis of galanthamine hydrobromide. By using plant Lycoris as the raw material, the method comprises the following steps of: raw material pretreatment, supercritical extraction, crude separation, purification, byproduct semi-synthesis and salifying crystallization. By using the supercritical extraction technology to carry out the extraction, the invention can effectively enhance the extraction efficiency and save the cost for reagent extracting; and by using macroporous adsorbent resin to carry out the crude separation and using a high-yield Sephadex LH-20 column to carry out the purification to obtain galanthamine of which the purity is greater than 98%, thereby greatly enhancing the separation efficiency and avoiding the environmental pollution. Simultaneously, the byproduct semi-synthesis step can make full use of byproducts obtained in the extraction process, thereby enhancing the utilization ratio of the raw material and the total yield of the process. Finally, the galanthamine hydrobromide of which the purity is greater than 99% is obtained after the salifying crystallization step. The invention has the advantages of reasonable concept, convenient method and easy popularization.

Description

technical field [0001] The invention belongs to a method for manufacturing chemical substances or medicines, and relates to a method for preparing galantamine hydrobromide, in particular a method for preparing and semi-synthesizing galantamine hydrobromide using plant Lycoris as raw material. Background technique [0002] A natural alkaloid, Galnathamine, as a cholinesterase inhibitor, comes from the Amaryllidaceae in the monocotyledonous plant. It was originally used for the treatment of myasthenia gravis and polio sequelae. To be used in clinical treatment of senile dementia, and the effect is obvious, almost no side effects. [0003] The molecular formula for galantamine is C 17 H 21 NO 3 , the molecular weight is 287.35, Chinese name: (4aS, 6R, 8aS)-4a, 5, 9, 10, 11, 12-hexahydro-3-methoxy-11-methyl-6H-benzofuran [3a, 3,2-ef][2]benzazepin-6-ol. [0004] To the best of the applicant's knowledge, galantamine is a potent, competitive and reversible inhibitor of acetylc...

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Problems solved by technology

[0013] The purpose of the present invention is to provide a method for preparing and semi-synthesizing galanthamine hydrobromide for the above-mentioned deficiencies in the prior art, so as to solve the problem that the existing extraction and preparation of galanthamine use a large amount of organic solvents and cause environmental problems. Pollution, high production costs and low efficiency, and comprehensive utilization of the by-products dihydrogalantamine and dihydroxygalantamine in the extraction process as much as possible, reuse them, and semi-synthesize galantamine, Solve the problem of low extraction yield of existing galantamine raw materials

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