3-亚甲基异吲哚啉-1-酮的硅氢化反应  

Hydrosilylation of 3-methyleneisoindolin-1-ones

作　　者：张晓梅 代兴杰 龙燕 王周玉 ZHANG Xiaomei;DAI Xingjie;LONG Yan;WANG Zhouyu(School of Science,Xihua University,Chengdu 610039 China)

机构地区：[1]西华大学理学院,四川成都610039

出　　处：《西华大学学报（自然科学版）》2020年第6期1-8,共8页Journal of Xihua University:Natural Science Edition

基　　金：国家自然科学基金资助项目(21672208)。

摘　　要：由于吲哚啉-1-酮单元广泛存在于各类天然产物及药物分子中,且3-取代异吲哚啉-1-酮对于天然产物的合成及新药研发具有重要价值;因此,化学家和药学家广泛关注3-取代异吲哚啉-1-酮合成方法。针对目前大部分合成方法反应条件苛刻、底物不易制备等问题,本文在易于合成的吡啶甲酰胺–磺酸酯类路易斯碱催化下,以廉价易得的三氯硅烷为还原剂,实现了3-亚甲基异吲哚啉-1-酮的硅氢化反应,以中等到优良的收率(63%~99%)得到了一系列3-甲基异吲哚啉-1-酮类化合物,从而找到了一种便捷、经济、环保的制备3-甲基异吲哚啉-1-酮类化合物的新方法。Isoindolin-1-one units exist in numerous natural products and biologically active substances.In addition,3-substituted isoindolin-1-ones are significant for the synthesis of natural products and development of new drugs.Therefore,the synthesis of isoindolin-1-ones has attracted extensive attention of chemists and pharmacologist.In order to solve the problems in many current procedures for the synthesis of isoindolin-1-ones such as harsh conditions and difficulties in preparation of substrates,in this paper,hydrosilylation of 3-methyleneisoindolin-1-ones has been achieved by using a readily available picolinamidesulphonate Lewis base as catalyst.The reaction provided a wide variety of 3-substituted isoindolin-1-ones in moderate to good yields(63%-99%).Thus,a facile,economic and environmental approach has been established for the preparation of 3-methyleneisoindolin-1-ones.

关 键 词：硅氢化 路易斯碱 3-亚甲基异吲哚啉-1-酮 3-取代异吲哚啉-1-酮 

分 类 号：O626[理学—有机化学] R914.4[理学—化学]