Copper-Mediated Bis(trifluoromethyl)carbinolation of Arylboronic Acids Enabled by Iodobis(trifluoromethyl)carbinol Ester

Organic Letters 2026

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Authors: Wenting Lai, Yahui Ding, Jie Ni, Shiqin Qiu, Rui Wang, Huaixuan Guo, Zhang Y, Peng Xu
DOI: 10.1021/acs.orglett.6c01500
Cited by: 1
References: 40

Abstract

The bis(trifluoromethyl)carbinol motif represents a privileged pharmacophore, yet its efficient construction, especially at a late stage, remains an unmet challenge. Here, we introduce iodobis(trifluoromethyl)carbinol ester (I-BTFCE) as a stable solid reagent that enables the hitherto Cu(I)-mediated bis(trifluoromethyl)carbinolation of arylboronic acids. This method provides streamlined access to diverse aryl bis(trifluoromethyl)carbinols, including natural product and pharmaceutical derivatives. The discovery of potent antiproliferative activity among the synthesized products highlights the significant biological potential of this synthetic method.

Fields of Study & Subjects

Fluorine in Organic Chemistry Catalytic C–H Functionalization Methods Catalytic Cross-Coupling Reactions

Publication details

Journal / source
Organic Letters
Publisher
American Chemical Society (ACS)
Volume
28
Issue
21
Pages
6672–6677
Publication date
14 May 2026
Language
EN