Study On Selection Of Synthetic Conditions Of Sotalol Hydrochloride In Class Ⅲ Antiarrhythmic Agents

Sotalol hydrochloride, naming (R,S)-(l-hydroxy-2-isopropyl amino)methylsulfonyl phenylamine hydrochloride in chemistry and setacor in trade, is an high effective non-heart selectivity #-blocket drug and has the third anti-arrhythymic drug characteristic. It has such advantages of strong function, extensive treatment area and little side effect that has get growing attentions.In this paper, Sotalol hydrochloride is fixed on our studying object on the basis of literature. Our aim is to obtain product in high yield and in accordance with raw drug quality standard though our research on technics and analyzing method.The product is synthesized from 4-nitroacetophenone via reduction to nitryl, methane sulfonylation with methylsulfonyl chloride, bromination with bromine, substitution with isopropylamine and reduction with KBH4.The best reaction condition is obtained though vast experiment and lucubrating to synthesis route. The solvent, temperature, material ratio, catalyzer, reaction time and disposing method are all improved to give reduced cost and high yield, the total yield has been raised to 43%.The dry weight loss, residue and other relative indexes are all excelling to the standard issued by department. IR spectrum is identical to the comparison. The content is high than 99.2%. The refined product is accord with raw drug quality standard.The improved synthesized method is simple, reliable and effective. The quality and yield of the product are very stable in repeating experiments, so the method is suitable for industrialization and has vast commercial foreground.