γ-氨基丁酸脂溶性前体药物合成及脂水分配系数测定

Synthesis of Liposoluble γ-Aminobutyric Acid Prodrug and Determination of Liposome-Water Partition Coefficient for It

目的合成γ-氨基丁酸脂溶性前体药物。方法以香豆素和γ-氨基丁酸为原料经过碱催化水解、乙酰化、醇解及DCC-HOB t活化酯法四步制备出目标化合物,并采用摇瓶法测定其在正辛醇/水中的分配系数。结果所得产物经熔点、红外谱图、核磁共振氢谱确证其结构,正辛醇/水分配系数为3.03。结论该合成方法简便易行,最终产物具有一定的脂溶性。

OBJECTIVE To Synthesize liposoluble γ- aminobutyric acid prodrug. METHODS Starting from coumarin and γ- aminobutyric acid,the target compound was prepared by base-catalyzed hydrolysis, acetylation, alcoholysis and activation method using DCC as the activating reagent in the present of HOBt in four steps, n-Octanol/Water partition coefficient was determined by shakingflask method. RESULTS The products were confirmed by melting point, IR and ^1H-NMR,the n-Octanol/Water partition coefficient was 3.03. CONCLUSION The synthetic method is simple,and the final product is liposoluble.