General and Scalable Approach to Trifluoromethyl-substituted Cyclopropanes

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

[2+2]-Photocycloaddition of <i>N</i>‑Benzylmaleimide to Alkenes As an Approach to Functional 3‑Azabicyclo[3.2.0]heptanes

A one-step synthesis of functionalized 3-azabicyclo[3.2.0]­heptanes by [2+2]-photochemical intermolecular cycloaddition of <i>N</i>-benzylmaleimide to alkenes was elaborated. The obtained compounds were easily transformed into the bi- and tricyclic analogues of piperidine, morpholine, piperazine, and GABA, which are advanced building blocks for drug discovery