A new synthesis method of esmolol hydrochloride

Esmolol hydrochloride is an ultra-short acting β₁-receptor blocker, which has mainly used for supraventricular tachycardia and perioperative hypertension. It has been also used for supraventricular tachyarrhythmia in clinical practice. The drug is characterized by quick effect and short action time. In this paper using 4-bromophenol as a starting material, esmolol hydrochloride was prepared by Heck reaction with methyl acrylate, hydrogenation, etherification with 3-bromopropene, oxidation, then isopropylamine was used to open the epoxide and salinization, the overall yield of the 6 synthetic steps is 46%. This method provides a new synthetic route for the synthesis of esmolol hydrochloride.