论文部分内容阅读
安定镇静药天麻素(对羟甲基苯-β-D-葡萄吡喃糖甙)为近年来由中药天麻中分离而得的主要有效成分之一,临床上现已用于治疗神经衰弱及血管性头痛等症。周俊等曾报道以葡萄糖为原料,经乙酰化、溴代、缩合、四氢硼钾还原、二次乙酰化、醇解等六步反应制得天麻素,总收率24％(对溴代四乙酰葡萄糖汁)。我们在该路线的基础上经过改进,用氢化还原代替四氢硼钾还原,如此可省去一步二次乙酰化和中间体四乙酰天麻甙的分离,简化了工艺,收率提高到31.8％。反应路线如下:
Sedative sedative gastrodin (p-hydroxymethylbenzene-β-D-glucopyranoside) is one of the main active components isolated from Gastrodia elata Blume in recent years and has been clinically used to treat neurasthenia and blood vessels Headache embolism. Zhou Jun et al. Reported that glucose was used as raw material, and gastrodin was obtained through six steps of acetylation, bromination, condensation, tetracyclic boron and potassium reduction, secondary acetylation and alcoholysis, with a total yield of 24% Tetraacetylglucose juice). On the basis of this route, we improved hydrogenation reduction instead of tetraborate potassium borate reduction, thus eliminating the need for one-step secondary acetylation and the separation of the intermediate tetraacetyl gastrodin, simplifying the process and increasing the yield to 31.8%. The reaction route is as follows: