异甘草素的简便合成研究  

Synthesis of Isoliquiritigenin

作　　者：黄继伟[1] 凌新龙[1] 林海涛[1] 

机构地区：[1]广西工学院生物与化学工程系,广西柳州545006

出　　处：《时珍国医国药》2012年第10期2454-2456,共3页Lishizhen Medicine and Materia Medica Research

基　　金：广西壮族自治区自然科学基金(No.2010GXNSFA013045);广西工学院科学基金项目(No.1074016)

摘　　要：目的研究异甘草素的合成工艺。方法以间苯二酚和对羟基苯甲醛为原料,通过乙酰化、羟基保护、羟醛缩合及脱保护合成得到了异甘草素,并对关键步骤羟醛缩合反应的条件(反应物的摩尔比、催化剂的种类、反应温度、溶剂和反应时间)进行了优化。结果以Ba(OH)2为催化剂,乙醇为反应溶剂,对羟基苯甲醛和2,4-二羟基苯乙酮的摩尔比为2.0,温度为78℃的条件下,反应24 h,异甘草素的合成收率最高,达到了86%。结论异甘草素的合成路线方便,原料简单,产率高。Objective To study the synthesis technology of isoliquiritigenin. Methods Isoliquiritigenin was synthesized with m - dihydroxybenzene and 4 - Hydroxybenzaldehyde as the starting materials by aeetylation, protecting of hydroxy, aldol condensation and deprotecting. The reaction conditions of the key step - aldol condensation, including ratio of reactants, catalyst, temperature, solvent and time were optimized. Results The optimal condition of the key step were as follows ： catalyst Ba （OH） 2, solvent EtOH, M （4 - Hydroxybenzaldehyde） ：M （2, 4 - Dihydroxyacetophenone） = 2.0, temperature 78℃ , and time 24 h. Under the optimal conditions, the yield of isoliquiritigenin was the highest and achieved 86%. Conclusion The synthetic route of isoliquiri- tigenin has advantages of convenience, simple raw materials and high yield.

关 键 词：异甘草素 生物活性 合成 

分 类 号：O629[理学—有机化学]