Stable BF₂ Boracycles as Versatile Reagents for Selective Ortho C-H Functionalization.

ABSTRACT: The development of new boron reagents continues to play a crucial role in advancing modern organic synthesis, particularly in C-H functionalization and cross-coupling reactions. Herein, we report a metal-free, robust, and scalable multigram protocol for the synthesis of stable BF₂ boracycles that require no column chromatography, providing a practical and efficient route to access this valuable boron species. The BF₂ boracycles exhibit enhanced stability and reactivity, making them highly versatile intermediates for late-stage diversification. They undergo ipso-substitution to afford a wide array of derivatives, including halogenated (e.g., radioiodinated), hydroxylated, and azidated products. Furthermore, they display excellent reactivity in Suzuki-Miyaura cross-coup

SUBMITTER: Shinde GH 

PROVIDER: S-EPMC12910154 | biostudies-literature | 2026 Feb

REPOSITORIES: biostudies-literature