3-亚甲基异吲哚啉-1-酮的硅氢化反应

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。

Hydrosilylation of 3-methyleneisoindolin-1-ones

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 picolinamide-sulphonate 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.