Research Antianginal Ivabradine Hydrochloride And Synthesis Of A New Generation Ceftaroline Fosamil

Ivabradine hydrochloride is the first selective and spccific I f channel inhibitor, andit is used for normal sinus rhythn, β-blockers contraindicated or intolerant chronic stable angina symptomatic treatment. Through the Food and Drug Administration of Europe approved, it listed in 27 countries in November 2005.Object The purpose of this study is to design industrial synthetic route by review the related literature, and analyze ivabradine hydrochloride’s quality, get the related impurities and determine the chemical structure of the relevant impurites.Methods 3,4-Dimethoxy-phenylacetic acid as the starting material, react with 2,2-dimethoxy ethylamine, to get N-(2,2-dimethoxyphenyl)-3,4-dimethoxy phenylacetamide. The compound cyclized under hydrochloric acid and acetic acid to get the seven-membered heterocyclic compound, which generate with 1-chloro-3-bromopropane and(1S)-4,5-dimethoxy-1-(methylaminomethyl) benzocyclobutene hydrochloride reaction of 3-[3-[[[(7S)-3,4-dimethoxy-bicyclo[4.2.0]oct-1,3,5-triene-7-yl]methyl]methylamino]propyl]-1,3-dihydro-2H-benzazepin-2-one, the resulting product is hydrogenated and soured by hydrochloric acid, the product obtained ivabradine hydrochloride.Results We get a more suitable synthetic route by different optimization of synthetic routes. Analysis of the final product obtained two new impurities that 3-(3-hydroxypropyl)-7,8-dimethoxy-1H-benzazepine-2(3H)-one(impurity A) and 3-(3-hydroxypropyl)-7,8-dimethoxy-4,5-dihydro-1H-benzazepine-2(3H)-one(impurity B) and get thetwo impurities by synthesis.Conclusion impurity A is generted 3-(3-chloropropyl)-7,8-dimethoxy-1H-benzoazpin-2(3H)-one by basic hydrolysis conditions. Impurity A reduction by hydrogen give impurity B. It is helps to avoid the formation of impurities in the production process to clear the impurities source, and providing control standards for final product.Ceftaroline fosamil belongs to the fifth generation cephalosporin antibiotic, it wasderived from a fourth-generation cephalosporins cefozopran. This topic through literature review, design the ceftaroline fosamil synthetic route and to give the product ceftaroline fosamil.