Characterization and Synthesis of A Betaxolol Hydrochloride Intermediate

摘要

In this paper, a new method was developed to synthesize betaxolol hydrochloride intermediate (1-[4-(2-Hydroxyethyl) phenoxy]-2, 3-epoxypropane). Based on the acidity difference of phenolic hydroxyl and alcoholic hydroxyl in p-hydroxyphenylethyl alcohol, the betaxolol hydrochloride intermediate was synthesized by selective A. W. Williamson etherification between p-hydroxyphenylethyl alcohol and epichlorohydrin in 18% potassium carbonate-acetone alkalescent solution. The molar ratio of p-hydroxyphenylethyl alcohol and epichlorohydrin was fixed at 1:1.7. FTIR and HPLC analysis revealed that the product purity reached 96% and the yield was 68.18%. This method simplified the synthetic process of betaxolol hydrochloride, which would also result in higher yield and purity of betaxolol hydrochloride products.