The Synthesis,Structure Confirmation And Qualitative Analysis Of Rupatadine Fumarate

Rupatadine fumarate is a new-type and highly potent antiallergic drug developed by Uriach pharmaceutical company in Spain.It has double effects of antihistamine and anti-platelet activating factor(PAF).In addition,the degranulation of mast cells,neutrophils and eosinophils,as well as mobile cytokine release are inhibited by this drug.Its major pharmacological function stems from Rupatadine,which has dual functions of antihistamine and anti-platelet activating factor(PAF).While Fumarate exerts the inhibiting effect on Colon Bacterium and Staphylococcus Aureus.Moreover,it can prevent tumor, inhibit electroshock and cough.So combination of Fumarate and Rupatadine increases the solubility of Rupatadine fumarate,facilitates assimilation by human body and decreases side-effects of Rupatadine fumarate.Rupatadine fumarate is the only drug in the market which has dual functions of antihistamine and anti-platelet activating factor(PAF),and thus it has the advantage over loratadine, the best-selling antihistamine in the world,and will become the first-line drug which can be used to cure allergic rhinitis,pneumonia and dermatosis. Consequently,research and development of this drug will have a promising market prospect.This experiment centers on the synthetic work,structure confirmation and qualitative analysis.The paper has two chapters,Chapter One,Synthesis and Chemical Structure Confirmaton of Rupatadine fumarate;Chapter Two,Qualitative Research on Rupatadine fumarate.Chapter one,in the field of synthesis of Rupatadine fumarate,we su mmarize the latest and optimal synthetic method of Rupatadine fumarate at home and abroad.The synthetic process used Loratadine and 3,5-dimethyl pyridine as raw materials,simplified the process and shortened the reactio n time.Then,compared with the standard reference in the same condition, elemental analysis,IR,UV,magnetic resonance,mass spectrometry were performed and analyzed for the structure confirmation of the sample.It is proved to be that the synthetic Rupatadine fumarate is a heterocyclic co mpound,containing benzene,pyridine ring,piperidine ring and two anti-aci d-based structure,and the sample' s molecule formula,molecule weight an d properties correspond with the standard reference,having no distinct diff erence.Chapter Two,in the qualitative research of Rupatadine fumarate,according to the Chinese Pharmacopoeia appendix requirements,the melting point, solubility,UV absorption coefficient and other physical and chemical constants of the Rupatadine fumarate were performed,the general and possible impurities were checked by HPLC,and a comprehensive study of the quality of samples were carried out,establishing a standard on the entire inspection and limited quantity.