This protocol demonstrates improved synthesis of functionalized quinolines, suggesting promise for antitumor applications.
Herein, we describe a B₂pin₂-mediated protocol for the synthesis of 2-difluoromethylthio/seleno-4-substituted quinolines via the cyclization of 2-alkenylanilines with TMSCF₃ and elemental sulfur or selenium. This method employs inexpensive and easy-to-handle TMSCF₃ as a dual C₁ and CF₂ 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.
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Dong et al. (2026) studied this question.
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