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Characterization and Synthesis of a Betaxolol Hydrochloride Intermediate
Abstract:
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.
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Pages:
770-773
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Online since:
January 2013
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