Current Topics in Medicinal Chemistry

Allen B. Reitz
Fox Chase Chemical Diversity Center, Inc.
Doylestown, PA


Decarboxylative Fluorination Strategies for Accessing Medicinally- Relevant Products

Author(s): Yupu Qiao, Lingui Zhu, Brett R. Ambler and Ryan A. Altman

Affiliation: Department of Medicinal Chemistry, the University of Kansas, 1251 Wescoe Hall Dr., 4046A Malott Hall, Lawrence, KS 66045, USA.

Graphical Abstract:


Fluorinated organic compounds have a long history in medicinal chemistry, and synthetic methods to access target fluorinated compounds are undergoing a revolution. One powerful strategy for the installation of fluorinecontaining functional groups includes decarboxylative reactions. Benefits of decarboxylative approaches potentially include: 1) readily available substrates or reagents 2) mild reaction conditions; 3) simplified purification. This focus review highlights the applications of decarboxylation strategies for fluorination reactions to access compounds with biomedical potential. The manuscript highlights on two general strategies, fluorination by decarboxylative reagents and by decarboxylation of substrates. Where relevant, examples of medicinally useful compounds that can be accessed using these strategies are highlighted.

Keywords: Decarboxylation, fluorination, difluoromethylation, trifluoromethylation, copper.

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Article Details

Page: [966 - 978]
Pages: 13
DOI: 10.2174/1568026614666140202210850