4.6 Review

Recent advances in the synthesis of pyrrolo[1,2-a]indoles and their derivatives

Journal

ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 19, Issue 35, Pages 7544-7574

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/d1ob01103k

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Funding

  1. CSIR, New Delhi
  2. SERB, New Delhi
  3. IIT Bombay

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The pyrrolo[1,2-a]indole unit is a privileged heterocycle found in numerous natural products and has diverse pharmacological properties. Recent years have seen significant interest in the synthesis of this scaffold, driven by the increasing demand for pyrrolo[1,2-a]indoles in drug discovery. This review provides an overview of recent synthesis methods for preparing pyrrolo[1,2-a]indoles and their derivatives, along with explanations on mechanistic pathways and stereo-electronic factors affecting product yield and selectivity.
The pyrrolo[1,2-a]indole unit is a privileged heterocycle found in numerous natural products and has been shown to exhibit diverse pharmacological properties. Thus, recent years have witnessed immense interest from the synthesis community on the synthesis of this scaffold. In light of the ever-increasing demand for pyrrolo[1,2-a]indoles in drug discovery, this review provides an overview of recent synthesis methods for the preparation of pyrrolo[1,2-a]indoles and their derivatives. The mechanistic pathway and stereo-electronic factors affecting the yield and selectivity of the product are briefly explained. Furthermore, we have attempted to demonstrate the utility of the developed methods in the synthesis of bioactive molecules and natural products, wherever offered.

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