INTRODUCTION OF PHOSPHATE GROUP INTO β-ARBUTIN BY CYCLO-TRIPHOSPHATE

Hideko Maeda, M. Katsushiro, H. Nariai, H. Nakayama
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Abstract

Phosphorylation of -arbutin has been achieved using inorganic cyclo-triphosphate (P3m) in aqueous solution. The optimum condition for the phosphorylation of -arbutin with P3m is -arbutin : P3m = 0.1 mol/L : 0.5 mol/L, pH 11 and 40oC. 4-Triphospho--arbutin was synthesized with the yield of 90%. The reaction mechanism of -arbutin with P3m was discussed. We have successfully introduced the triphosphate group in one molecule. Phosphorylated -arbutin is expected that the permeability of -arbutin into the skin will be increased by introducing a phosphate group. (Received Jul 7, 2017; Accepted Aug 2, 2017)
环三磷酸法将磷酸基团引入β-熊果苷
利用无机三磷酸环(P3m)在水溶液中实现了-熊果苷的磷酸化。P3m磷酸化-熊果苷的最佳条件为-熊果苷:P3m = 0.1 mol/L: 0.5 mol/L, pH为11,温度为40℃。合成了4-三磷酸-熊果苷,收率达90%。探讨了-熊果苷与P3m的反应机理。我们已经成功地在一个分子中引入了三磷酸基团。磷酸化-熊果苷,预计-熊果苷对皮肤的渗透性将通过引入磷酸基团而增加。(2017年7月7日收稿;2017年8月2日录用)
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