Method for preparing transdermal absorption synephrine derivative

Abstract

The invention discloses a method for preparing a transdermal absorption synephrine derivative, and relates to a method for preparing acetylation synephrine. The method takes synephrine sold on the market as a raw material, and a product is obtained through acylation reaction, silica column chromatography, nanofiltration, freeze drying and vacuum filtrating and drying. The method is simple, convenient to operate, simple in production equipment, moderate in reaction condition, safe to produce and low in production cost; an acetylation synephrine product and a calcium acetate byproduct with high purity and high yield can be produced; and pyridine and n-butyl alcohol can be recycled, material resources are fully utilized, 'three wastes' emission is not generated, green production can be realized and the like. The method can be widely used for producing the acetylation synephrine product; and the product produced according to the invention can be widely used for weight losing medicines and health-care products, and the produced calcium acetate byproduct can be widely used in the fields of chelating agents, enzyme inhibitors, stabilizers and the like.

Description

1. Technical field [0001] The invention belongs to the technical field of chemical modification of plant extracts, in particular to a preparation method of synephrine derivatives (ie, acetylated synephrine). 2. Background technology [0002] Obesity is one of the major problems plaguing human health in the 21st century. Because the active ingredients ephedrine, pseudoephedrine and caffeine of traditional weight-loss drugs have the risk of inducing diseases such as stroke, heart disease and high blood pressure, in 2004 the U.S. Food and Drug Administration issued a regulation on ephedrine and other dietary supplements. In August 2012, China's State Food and Drug Administration issued a notice that it would no longer approve the registration of generic drugs containing ephedrine-based compound preparations, and restrict the sales of ephedrine products with minimum packaging specifications. Therefore, finding new plant extracts with slimming effect has become an urgent problem...

AI Technical Summary

Problems solved by technology

The main disadvantages of this method are: 1. Hydrogen chloride needs to be continuously fed into the acylation reaction, which is difficult to operate, high in risk, and unfriendly to the environment; 2. The reduction reaction requires noble metals as catalysts, which increases production costs; Large investment, high operation and maintenance costs, further increasing production costs; ④ incomplete reaction, poor specificity, close properties of raw materials and product mixtures, difficult purification in the later stage, and poor product quality; ⑤ chemically synthesized synephrine may remain Toxic and harmful substances such as phenol are difficult to be used in industries such as medicine and have poor practicability