无溶剂硼酸高效合成螺杂双环衍生物  

Efficient Solvent-free Synthesis of Spiro Heterobicyclic Derivatives with Boric Acid as Catalyst

作　　者：许招会[1] 刘德勇[1] 涂缘鸿 

机构地区：[1]江西师范大学国家单糖化学合成工程技术研究中心,南昌330027

出　　处：《应用化学》2015年第9期999-1004,共6页Chinese Journal of Applied Chemistry

基　　金：国家科技攻关计划(2001BA323C);江西省研究生创新基金(YC2015-B030)资助项目~~

摘　　要：在硼酸催化下,芳香醛、尿素和2,2-二甲基-1,3-二噁烷-4,6-二酮在无溶剂条件下合成了8种螺杂双环衍生物。当催化剂的用量为10%（摩尔分数）时,80℃反应2.0~4.0 h,收率为74%~93%。此外,还探讨了硼酸可能的催化机理。该方法具有条件温和,后处理工艺简单及收率高的优点。Eight spiro heterobicyclic compounds were synthesized by the three component condensation reaction of aromatic aldehydes with urea and 2,2-dimethyl-1,3-dioxane-d ,6-dione using boric acid as catalyst under solvent-free conditions. The results indicate that the yields range from 84% to 94% at 80℃ for 2. 0 4.0 h using 10% molar fraction of boric acid （ relative to the substrate of 2,2-dimethyl-1,3-dioxane4,6- dione）. Furthermore, a mechanism for the reaction catalyzed by boric acid was proposed. The main advantages of the present procedure are mild conditions, short reaction time and high yields.

关 键 词：硼酸 无溶剂 三组分反应 螺杂双环衍生物 

分 类 号：O625.3[理学—有机化学]