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. 2023 Mar 17;88(6):3859-3870.
doi: 10.1021/acs.joc.3c00123. Epub 2023 Feb 24.

General and Scalable Approach to Trifluoromethyl-Substituted Cyclopropanes

Volodymyr Ahunovych  1   2 , Anton A Klipkov  1   2 , Maksym Bugera  1   2 , Karen Tarasenko  1   2 , Serhii Trofymchuk  1   3 , Oleh Stanko  1 , Andrii Boretskyi  1 , Mykola Zheludenko  1 , Iryna V Sadkova  1 , Pavel K Mykhailiuk  1
Affiliations

General and Scalable Approach to Trifluoromethyl-Substituted Cyclopropanes

Volodymyr Ahunovych et al. J Org Chem. .

Abstract

CF3-cyclopropanes with aliphatic, aromatic, and even heteroaromatic substituents were prepared on a multigram scale by deoxyfluorination of cyclopropane carboxylic acids or their salts with sulfur tetrafluoride. For labile α-pyridine acetic acids, only the use of their potassium salts allowed to obtain the needed products. Derivatization of CF3-cyclopropanes into building blocks ready for direct use in medicinal chemistry was performed.

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