A practical metal-free homolytic aromatic alkylation protocol for the synthesis of 3-(pyrazin-2-yl)bicyclo[1.1.1]pentane-1-carboxylic acid.

As a part of our ongoing synthetic quest to expand the frontiers of contemporary medicinal chemistry, we now report an expedient synthesis of a potentially useful bicyclo[1.1.1]pentane building block, 3-(pyrazin-2-yl)bicyclo[1.1.1]pentane-1-carboxylic acid. This report also showcases the application of this motif as a probe in a biological study.

Expedient synthesis of 3-phenylbicyclo[1.1.1]pentan-1-amine via metal-free homolytic aromatic alkylation of benzene.

Recently, the potential utility of the BCP motif, as a contemporary lead optimization tactic, has generated substantial interest in medicinal chemistry. To facilitate this inquisitiveness, the concomitant development of efficient synthetic protocols is crucial. The following work discloses a new, expedient and versatile approach to one such potentially useful BCP derivative.