全反式维甲酸四乙酰葡萄糖酯的合成及急性皮肤刺激性研究

STUDIES ON SYNTHESIS AND ACUTE SKIN IRRITATION OF 1-O-RETINOYL- D-GLUCOPYRANOSE TETRAACETATES

全反式维甲酸在４－二甲氨基吡啶催化下，与２，３，４，６－四－Ｏ－乙酰－α－Ｄ－吡喃葡萄糖溴化物反应，生成全反式维甲酸四乙酰葡萄糖酯（１），收率５８％ 。急性皮肤刺激试验表明：１ 对皮肤刺激性小于全反式维甲酸（２），而且保持与全反式维甲酸一样的生物活性。

O all trans Retinoyl D glucopyranose tetraacetate (1) was obtained by the condensation of 2,3,4,6 tetra O acetyl D glucopyranosyl bromide (3) with all trans retinoic acid (2) in the presence of 4 dimethylaminopyridine as catalyst, 1% potassium hydroxide and dichloromethane at 40°C, and the yield was 58%. The acute skin irritation of 1 was less than that of 2.