Green synthesis for diverse bioactive benzo-fused spiroindolines through DBU-catalysed post-Ugi double cyclization†
Zhenghua
Li, 
c
Shenyou
Nie
*ab
and
c
Shenyou
Nie
*ab
and
Abstract
A metal-free protocol utilizing DBU catalysis for post-Ugi amide-ester exchange and Conia-ene double cyclization has been successfully developed, allowing the synthesis of diverse highly functionalized benzo-fused spiroindolines with anti-cancer activities under mild conditions. Remarkably, this methodology demonstrates promising prospects for green chemistry, as it allows for the preparation of the spiroindolines in water. Control experiments indicate that a crucial role of the cyclic imide, specifically ring rigidification, facilitates the subsequent Conia-ene cyclization.
- This article is part of the themed collection: CC 60th Anniversary Authors Collection
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