超声辅助铜催化合成α-卤代甲基酮  

Synthesis of α-Halomethylketones by Ultrasound-promoted Copper-catalysis

作　　者：兰立新[1] 肖洁[1] 鄢东[1] 易卫国[1] LAN Li-xin;XIAO Jie;YAN Dong;YI Wei-guo(College of Chemical Engineering, Hunan Chemical Vocational Technology College, Zhuzhou 412000, China)

机构地区：[1]湖南化工职业技术学院制药与生物工程学院

出　　处：《化学试剂》2018年第4期403-406,共4页Chemical Reagents

基　　金：湖南省教育厅科学研究资助项目(15C0464)

摘　　要：α-卤代甲基酮不仅是有机合成的重要中间体,也是许多药物分子中的重要结构片段。发展了超声辅助下铜催化卤代炔烃水合反应制备α-卤代甲基酮化合物的新方法。考察了催化剂的种类、酸的种类、反应温度以及溶剂对反应的影响。研究结果表明,在超声条件下,以5 mol%Cu（OTf）2为催化剂,40℃反应1 h,卤代炔烃能够以良好的反应产率得到水合产物α-卤代甲基酮。所得产物结构均经过1HNMR、13CNMR和MS表征。本反应方法简单、条件温和且收率良好,提供了一种合成α-卤代甲基酮的新方法。α-Halomethylketones are very improtant synthetic intermediates as the building blocks for the synthesis of various drug molecules.A novel ultrasound-promoted highly efficient synthesis of a wide range of α-halomethylketones from haloalkynes is described.The influences of catalyst,acid,reaction temperature and solvent were investigated,the result indicated that the reaction proceeds smoothly to give the corresponding products in good yields using 5 mol% Cu（ OTf）2 for 1 h at 40 ℃.The structure of α-halomethylketone derivatives was confirmed by1 HNMR,13 CNMR and MS.The reaction method with its advantages of simple procedure,mild reaction conditions and high yield provides a novel valuable approach to α-halomethylketone.

关 键 词：水合反应 铜催化 超声 α-卤代甲基酮 

分 类 号：O621.25[理学—有机化学]