B 2 pin 2 -Mediated Cascade Cyclization of 2-Alkenylanilines To Give 2-Difluoromethylthio/seleno-4-Aryl(alkyl)-Quinolines
Abstract
Herein, we describe a B 2 pin 2 -mediated protocol for the synthesis of 2-difluoromethylthio/seleno-4-substituted quinolines via the cyclization of 2-alkenylanilines with TMSCF 3 and elemental sulfur or selenium. This method employs inexpensive and easy-to-handle TMSCF 3 as a dual C 1 and CF 2 source for the efficient construction of highly functionalized quinolines. The reliability, practicality, and scalability of this process are fully demonstrated through gram-scale synthesis, late-stage functionalization, and evaluation of its potential antitumor activity.
Fields of Study & Subjects
Fluorine in Organic Chemistry
Sulfur-Based Synthesis Techniques
Click Chemistry and Applications
Publication details
- Journal / source
- Organic Letters
- Publisher
- American Chemical Society (ACS)
- Volume
- 28
- Issue
- 15
- Pages
- 4841–4846
- Publication date
- 1 April 2026
- Language
- EN