Studies On Synthesis And Quality Standard Of Esomeprazole Sodium

Esomeprazole, being the s-type optic isomer of Omeprazole,which was the first marketed proton pump inhibitor,which inhibiting of parietal cell proton pump to reduce gastric acid secretion through specific,suitable for gastroesophageal reflux disease, esomeprazole was an effective treatment with inhibiting gastric acid than that of omeprazole and other marketed proton pump inhibitor, and had a better clinical therapeutic effect of acid correlation disease.Because of the traditional synthetic route contains complex procedures,low yields,highly difficult purification technical and high cost,this paper focused on the optimization of synthesis process which was the main target,especially studied the reaction conditions of asymmetric oxidation and refining,the suitable process condition of product were obtained and successfully got through the scale-up validation. The whole process became more simply,the condition became more mild, and the yield and purity of products were significantly improved. The structure of products were confirmed by the means of NMR,MS, IR and UV.Quality standards aspects:the different properties of the products were researched: appearance properties, solubility, moisture absorption,optical rotation, identification, alkalinity, absorbance, heavy metal,related substances, isomers and content. Meanwhile,the specificity,linearity, stability, and accuracy were studied with the properties by the means of methodology methods. The results showed the methods were effective for the quality control with raw materials of esomeprazole.