作者简介:刘亚玲(1990-),女,湖南长沙人,在读研究生。E-mail:310231372@qq.com 。脱氧熊果苷的合成1. 浙江工业大学药学院,浙江杭州310014;2. 浙江工业大化学工程学院,浙江杭州 310014 摘要: 结合脱氧熊果苷合成的单缩合法和三步法,对已有文献的方法进一步试验和优化,提出了以对苯二酚和乙酰氯为原料,通过乙酰氯单保护,然后与3, 4-二氢吡喃反应生成四氢吡喃醚, 最后利用硼酸钠脱乙酰基得到脱氧熊果苷的合成路线。同时将该合成路线中的反应时间,催化剂用量,物料比等影响因素进行优化,优化后三步产率分别为83.4%,83.9%,80.4%。该路线反应条件简单,三步皆在常温常压下反应;用廉价的硼酸钠作为催化剂,工业化成本低; 三步反应用的催化剂都是一些常见的盐,避免使用了重金属对环境的危害,且过量的对苯二酚回收充分,废液污染少。关键词: 脱氧熊果苷;对苯二酚;乙酰氯;合成A Study on the Synthesis of Deoxyarbutin LIU Ya-ling1,LI Kang-wu 1,WANG XX 2 1.College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, China ;2.College of Chemical Engineering and Materials Science, Zhejiang University of Technology, Hangzhou 310014, ChinaAbstract:A new synthetic route of deoxyarbutin has been designed on the base of previous procedure, meanwhile, the influencing factors have been optimised, with yields of 83.4%, 83.9% and 80.4% for each step. Deoxyarbutin is synthesized by deacetylation of 2-[(4-acetyloxy)]tetrahydropyran, with the sodium borate, which is an intermediate obtained by condensation of 3,4-dihydropyran and monoacetyhydroquinone. The procedure of the recent route is easy to operate, and all the three steps proceed well at room temperature. The synthetic costs are low as cheap catalysts are used. Key words:deoxyarbutin ;hydroquinone;acetylchloride ;synthesis 熊果苷类美白添加剂是目前国内外常用于美白化妆品中的主要原料[1],相对于氢醌长期使用对机体产生损伤而言[2],熊果苷类产物具体有更高的安全性,国际上已有多个国家将它们应用到化妆品中[3]。根据实...