General and Scalable Approach to Trifluoromethyl-Substituted Cyclopropanes

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.