Cholinesterase inhibitor preparation method

Abstract

The invention discloses a cholinesterase inhibitor preparation method, and belongs to the technical field of separation and purification of natural medicines. The preparation method comprises: soakinga macroporous cation exchange resin by using an acid solution, completely removing the acid liquid, rinsing with water, soaking with an alkali liquid, rinsing with water, soaking with an acid liquid,rinsing with deionized water, and replacing with lower alcohol; adding glycerol phosphate to the lower alcohol, adding an alkali, carrying out a reaction, carrying out suction filtration, washing with lower alcohol, adjusting the pH value to a weakly alkaline state, carrying out pressure reducing concentrating, cooling, transferring into a separatory funnel, standing, and separating to obtain a lower layer lower alcohol phase; loading glycerol phosphate and a phenol formaldehyde resin onto a column, loading the alcoholysis mixing liquid onto the column, adsorbing, washing the resin with loweralcohol to remove impurities, and eluting the resin with pure water; and decolorizing with a decolorizing agent, and carrying out pressure reducing concentrating to obtain the finished product. According to the present invention, the process steps are short, the requirements of industrial production are met, the resources are saved, the cost is reduced, the total yield of the finished products is65.47-86.08%, the external standard content is over 99%, and the optical purity is 99%.

Description

technical field [0001] The invention belongs to the technical field of separation and purification of natural medicines, and in particular relates to a preparation method of a cholinesterase inhibitor. Background technique [0002] Glycerol phosphatidylcholine (English name: new glycerophosphorylCholine, abbreviated as new GPC) is a naturally occurring water-soluble phospholipid metabolite in the human body, and it is also a precursor for the synthesis of acetylcholine and phosphatidylcholine (PC). Its structure consists of choline , glycerol and phosphatidyl groups. The new GPC is a cholinesterase inhibitor, which can effectively prevent and treat cerebral ischemic stroke. It can not only improve the memory and cognitive ability of patients, treat Alzheimer's disease and cranial nerve injury, but also resist Muscle atrophy, resist hyperlipidemia and arteriosclerosis, protect blood vessels, etc., so it is widely used in medicine and health care products and other industries...

AI Technical Summary

Problems solved by technology

In 1954, U.S. Patent No. 2,864,848 disclosed a mercury salt precipitation method, which was to precipitate by-products in the form of mercury salts, and remove excess mercury ions by hydrogen sulfide and barium carbonate, but it was difficult to fully remove mercury ions, due to the residual Reactive PC, so it is necessary to add calcium salt to precipitate the new GPC to remove mercury ions, and finally use resin to remove calcium salt

It can be seen that the efficiency of this method is low, the process is more complicated, and the final yield is not ideal

Subsequently, Brockerhoff used the recrystallization method to prepare a new type of GPC pure product, but the catalyst needs to be removed, and the product is recrystallized and purified. The whole process is more complicated and costly, and it is not suitable for commercial scale production.