An efficient method for preparation of substituted 6H-isoindolo[2,1-a]indol-6-ones (2) that are important structural components of a vast array of naturally occurring and pharmacologically active compounds, has been developed by the palladium-catalyzed intramolecular cycloaminocarbonylation of 2-(1H-indol-2-yl)phenyl tosylates with CO. Significantly, the intermolecular aminocarbonylation products 2-(1H-indol-2-yl)benzamides are formed when an excess of amine is used in this reaction system. Alternatively, 2-(1H-indol-2-yl)benzamides can also be synthesized by the in situ aminolysis of 2. Furthermore, treatment of 2 with hydrosilane in the presence of KOH gave the unprecedented reducing products 2-(-1H-indol-2-yl)benzyl alcohols in 75–86% yields. These results demonstrate that 6H-isoindolo[2,1-a]indol-6-ones are versatile substrates for further synthetic elaboration.

钯催化开发了一种有效的制备取代的6H-异吲哚并[ 2,1 - a ]吲哚-6-酮（2）的有效方法，该取代的6H-isoindolo [ 2,1 - a ]吲哚-6-酮是大量天然存在的药理活性化合物的重要结构组分。的分子内cycloaminocarbonylation 2 - （1H-吲哚-2-基）苯基甲苯磺酸酯用CO值得注意的是，分子间氨基羰基化产物2 - （1H-吲哚-2-基）当过量的胺在该反应系统中使用形成的苯甲酰胺的。或者，还可以通过2的原位氨解来合成2-（1H-吲哚-2-基）苯甲酰胺。而且，治疗2在KOH的存在下与氢硅烷反应，以75-86％的收率得到了空前的还原产物2 -（-1H-吲哚-2-基）苄醇。这些结果证明6H-异吲哚并[2，1- a ]吲哚-6-酮是用于进一步合成加工的通用底物。