General and Scalable Approach to Trifluoromethyl-substituted Cyclopropanes

18 January 2023, Version 1
This content is a preprint and has not undergone peer review at the time of posting.

Abstract

CF3-cyclopropanes 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 salts allowed to obtain the needed products. Derivatization of CF3-cyclopropanes into building blocks ready for the direct use in medicinal chemistry was performed.

Keywords

cyclopropanes
trifluoromethyl
tetr-butyl
bioisosteres
medicinal chemistry

Supplementary materials

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