改良Wittig反应在生物活性化合物合成中的应用进展  

Research Advances on the Applications of Improved Wittig Reactions in the Synthesis of Biologically Active Compounds

作　　者：周艳斐[1] 郑土才[1] 史芳芳[1] 叶山海 王小青 

机构地区：[1]衢州学院化学与材料工程学院,324000 [2]浙江海昇化学有限公司,浙江衢州324004

出　　处：《化工生产与技术》2014年第2期46-56,69,共11页Chemical Production and Technology

基　　金：衢州市科技计划项目(20121040)

摘　　要：介绍了改良Wittig反应的特点,叙述了改良Wittig反应在生物活性化合物合成中的应用,分别归纳了酯、腈、酰胺、酮等α位、烯丙位、苄位和其他膦酸酯的改良Wittig反应及其用碱、溶剂等条件,并介绍了改良Wittig反应在农药合成中的应用。认为制备膦酸酯的方法也可以使用偕二膦酸酯、乙二膦酸酯等与醛酮反应制得,也可使用活泼氢金属化后与二烷氧基磷酰氯缩合制得,或使用由简单膦酸酯经α烃基化制得的复杂膦酸酯等;应重点研究价廉易得的碱及相转移催化下的固体氢氧化钠或氢氧化钾或其水溶液,并加强改良Wittig反应的工业化研究。This review introduced the characteristics of the improved Wittig reaction,summarized the applications of improved Wittig reactions in the synthesis of biologically active compounds,respectively summarized the improved Wittig reactions of alpha site,allyl site,benzyl site from ester,nitrile,amide,ketone and other phosphonate,and the alkali using,solvents and other conditions,and also introduced the application in the synthesis of pesticides.The phosphonate could also be prepared by bisphosphonate and ethyl bisphosphonate with aldehyde and ketone,or be condensation prepared by lively hydrogen after metallization with two alkoxy phosphorus oxychloride,or complex phosphonate was prepared through alpha alkyl from simple phosphonate.Research should focus on cheap alkali and solid sodium hydroxide or potassium hydroxide or its aqueous solution in phase transfer catalysis and strengthen the industrial research of improved Wittig reaction.

关 键 词：改良Wittig反应 Horner反应 Arbuzov重排 膦酸酯 亚磷酸三乙酯 合成 

分 类 号：TQ203.9[化学工程—有机化工]