Rapid Access to Diverse Potassium Acyltrifluoroborates (KATs) Through Late-Stage Chemoselective Cross-Coupling Reactions

18 November 2020, Version 1
This content is a preprint and has not undergone peer review at the time of posting.


Potassium acyltrifluoroborates (KATs) are opening up new avenues in chemical biology, materials science and synthetic organic chemistry due to their intriguing reactivities. However, the synthesis of these compounds remains mostly complicated and time-consuming. This lack of a rapid and facile synthetic route has hindered the widespread adoption of KAT-based chemistry, especially in the areas of compound library synthesis and drug discovery. Herein, we have developed chemoselective Pd-catalyzed approaches for the late-stage diversification of arenes bearing pre-functionalized KATs. These approaches feature chemoselective cross-coupling, rapid diversification, functional group tolerance, mild reaction conditions, and high yields.


late-stage modification
Suzuki Coupling
Buchwald-Hartwig amination
sonogashira coupling
Heck coupling
chemoselective cross-coupling
potassium acyltrifluoroborates
KAT ligation

Supplementary materials

Supporting Information-17 Nov


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