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Dearomative Indole Annulation with 2-Aminoaryldisulfide - an Approach for Accessing Polycyclic
Sudipta Baur1, Sayari Chanda1, Joydev K Laha1
1Department of Pharmaceutical Technology (Process Chemistry), National Institute of Pharmaceutical Education and Research, S. A. S. Nagar, Mohali, Punjab 160062, India.
Organic Letters
|February 14, 2026
Summary
We developed a new method for synthesizing complex 3D indoline frameworks from indoles and disulfides. This efficient protocol is useful for modifying drugs and natural products.
Area of Science:
- Organic Chemistry
- Synthetic Chemistry
Background:
- Indoline frameworks are important scaffolds in medicinal chemistry.
- Efficient synthesis of 3D indoline derivatives remains challenging.
Purpose of the Study:
- To develop a practical protocol for the dearomative annulation of indoles with 2-aminoaryl disulfides.
- To access diverse three-dimensional (3D) indoline frameworks.
Main Methods:
- Dearomative annulation reaction.
- Utilized 2-aminoaryl disulfides and indoles.
- Employed N-fluorobenzenesulfonimide (NFSI) for activation.
Main Results:
- Achieved synthesis of 3D indoline frameworks under mild conditions.
- Demonstrated remarkable functional group tolerance.
- Successfully applied the method for late-stage modification of drugs and natural products.
Conclusions:
- The developed protocol provides an efficient route to complex indolines.
- The method's functional group tolerance and applicability in late-stage modification highlight its utility in drug discovery and natural product synthesis.
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