Method for fully synthesizing berberine

Abstract

The invention discloses a method for fully synthesizing berberine, and relates to a drug synthesis method. The method realizes the industrial full synthesis production of the berberine and is made from a bulk organic raw material catechol, the raw material is easily available, and the price is low; 2,3-dimethoxybenzaldehyde is obtained through selective formylation and methylation of the catechol;after a piperonyl ring is obtained through a catechol methylenenation reaction, piperonyl amine is synthesized through a one-step catalytic addition reaction, so that the synthesis steps of the piperonyl amine are shortened, the use of toxic cyanide is avoided, and the process is green and sustainable; condensation hydrogenation and salification reactions adopt a 'one-pot method', and thus the time and the energy are saved, and the cost is decreased. Industrialized full synthesis production of the berberine opens up large-scale production of the berberine, meets the clinical and research needs of the berberine in current anti-tumor, anti-blood pressure, anti-heart rhythm, blood sugar reduction, treatment of Alzheimer's disease and the like, provides effective drugs for reducing pain of patients, and has remarkable economic and social benefits.

Description

technical field [0001] The invention relates to a method for synthesizing medicine, in particular to a method for fully synthesizing berberine. Background technique [0002] Berberine hydrochloride (berberine), also known as berberine hydrochloride, is a yellow needle-like crystal, its molecular formula (excluding crystal water) is C20H18ClNO4, its molecular weight is 371.8, and its melting point is 145°C. The industrial product contains 2-5 molecules of crystal water, which can be Soluble in hot water, ethanol, insoluble in ether, benzene. It is a light yellow powder under normal conditions, and becomes earthy yellow after being heated and dehydrated. Hydrochlorides are poorly soluble in water but readily soluble in hot water, while sulfates are easily soluble in water. Berberine is a quaternary ammonium isoquinoline alkaloid with a nitrogen triangle chemical structure. Berberine is a yellow extract from plants of the genus Berberis, which was first discovered by Buchner...

AI Technical Summary

Problems solved by technology

The chemical synthesis technology of berberine hydrochloride has achieved industrial mass production. However, there are still some shortcomings in the process, such as the use of toxic substance cyanide, many reaction steps, low yield, and unclear related substances. Continue to carry out technological innovation and strengthen the existing process Research on the reaction mechanism and key technologies of technology is a top priority to ensure product output and quality, and to reduce costs and increase benefits

[0004] Using ortho-vanillin as raw material, the production capacity of berberine hydrochloride is limited by the production capacity of vanillin. On the one hand, as a by-product of vanillin, there is only a small amount of industrial supply, and the production capacity cannot be enlarged. On the other hand As a by-product of vanillin, its impurity composition and content have not been effectively controlled. Seeking alternative raw materials for ortho-vanillin will innovate the berberine process technology route

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