Quality Standard Research Of EBTP API

Erianin is a diphenylethane compound with natural anti-tumor active ingredients extracted from the traditional Chinese medicine Dendrobium.Previously,our research group used Erianin as the lead compound to modify the structure and discovered a new drug candidate compound EBT with intellectual property rights.In this paper,a synthetic method of EBTP bulk drug was developed,and the key phosphate salt formation step was improved.The impurity spectrum analysis of the EBTP bulk drug was carried out,the reference substance of related substances was synthesized,and the EBTP bulk drug was preliminary Quality research.The first part is to develop a new synthetic method of EBTP bulk drug.Stilbene acrylic acid was constructed through Perkin reaction,which was hydrolyzed into dibenzyl ketone after Curtius rearrangement,and Huang Minglong was reduced to diphenylethane,and the precursor was formed by hydrogenation and debenzyl protection.EBT.In order to increase the water solubility,the phenolic hydroxyl group is formed into a phenol phosphate salt,the precursor EBT is reacted with pyrophosphoryl chloride,a fulric acid agent is added during the reaction,and a post-treatment is used to obtain disodium phosphate EBTP.The optimal reaction conditions were obtained by screening the amount of glutenic acid agent,the reaction temperature,the amount of pyrophosphoryl chloride,and the reaction time.Compared with others,the synthesis method has simple steps,mild reaction conditions,and high reaction yield.The second part is to synthesize the relevant impurities of EBTP.At present,we still use the method that has been verified by pilot scale-up to synthesize EBTP.The EBTP product may contain organic impurities mixed into the finished product,which will affect the safety and safety of the drug in clinical use.Effectiveness.In order to carry out the quality research of related substances in the follow-up,this article will synthesize the reference substance of EBTP related impurities and confirm its structure through spectral analysis to confirm that the structure meets expectations.The third part is about the quality research of EBTP raw materials.The quality research of drugs is an important part of ensuring the safety and effectiveness of drugs.This article conducts the necessary quality of EBTP raw materials through physical and chemical properties investigation,identification,inspection and stability investigation Research and stability studies,in order to provide a reference for its storage conditions,found that the EBTP bulk drug is more sensitive to acid and high temperature conditions.