An efficient route to prepare the 4-hydroxy-2,3,4,5-tetrahydro[1,4]diazepino[1,2-a]indol-1-one scaffold is described. The key reactions of the synthesis are an iodolactonisation followed by a lactone-to-lactam rearrangement. Various 11-substituted derivatives were obtained by palladium-mediated cross-coupling reactions.
一种高效制备
4-羟基-2,3,4,5-四氢[1,4]二氮杂卓[1,2-a]
吲哚-1-酮骨架的方法被报道。合成中的关键反应包括
碘内酯化反应和内酯至内酰胺的重排。通过
钯介导的交叉偶联反应,得到了多种11-取代衍
生物。