盐酸索他洛尔的合成

Synthesis of Sotalol Hydrochloride

苯胺与甲磺酰氯反应得到N-苯基甲磺酰胺,然后与氯乙酰氯进行酰化反应得到N-[4-(2-氯乙酰基)苯基]甲磺酰胺,随后经异丙胺化得到N-[4-(2-异丙胺基乙酰基)苯基]甲磺酰胺盐酸盐,最后经还原反应后成盐制得盐酸索他洛尔,总收率约64%(以苯胺计)。

After the reaction with mesyl chloride, aniline was converted into N-phenylmethanesulfonamide, which was reacted with chloroacetyl chloride to afford N-[4-（2-chloroacetyl）phenyl] methanesulfonamide （3）. Sotalol hydrochloride was finally synthesized from isopropylamination of compound 3 followed by reduction and salification with an overall yield of about 64 % （based on aniline）.