Pantoprazole Sodium Synthesis Process

In recent years,proton pump inhibitors(PPI)has become the mainstream drug for the treatment of Gastric ulcer disease.Pantoprazole sodium is omeprazole,lansoprazole listed after the third proton pump inhibitor.In 1994,Germany 100 grams of Dayton(BydGulden)company first successfully developed and listed in South Africa,has been in the United States,Britain,Germany and other countries allowed more than 20.Listed with other proton pump inhibitors,pantoprazole sodium is the weak acidic conditions stable,the conditions in the acidity soon be activated with other drugs mutual small role,.The papers major researchs the pantoprazole sodium in the synthesis conditions,and the technical level has reached the international advanced level.Through research on the first five industrialized reference value with the synthetic route,then under laboratory conditions groping a detailed description of a reasonable Process;Domestic maltol (2-Methyl-3-hydroxy-4-pyranone)as raw material,through methylation reaction,amination reaction,chlorination,oxidation reaction, methoxy-reaction,rearrangement,the hydrolysis reaction, chlorination,condensation,oxidation,salt reaction.Total 10 step reaction in pantoprazole sodium monohydrate,an overall yield of 30%, higher than the reported literature the yield Road.This paper describes in detail the various steps of the process conditions,discussed and compared the impact of product quality and yield of the main factors that draw the best reaction conditions.The main thesis of this innovation;1)Preparation of the compound(2),in the course of phase transfer catalyst under the conditions of use of dimethyl carbonate as methyl green reagent can not only enhance the yield and improve the labor environment,stop by dimethyl sulfate lethal diseases caused by the occurrence;2)oxidation reaction,the preparation of compounds(4)and compound (1)the process of peroxyacetic acid used instead of M-choroperoxybenzoic acid,oxidizer intensity,high yield and purity of the product was to get better control;3)Preparation of the compound(5)process,the use of cuprous ion catalyst under the conditions of high pressure reactor for methicillin-based,the product was to be a corresponding increase;4)rely on the compound(10)and compound(1)when the salt into the different nature and effectively remove impurities compounds(10).