3,3-BIARYLPROPYLAMINES: A STRAIN-RELEASE STRATEGY FOR MODULAR SYNTHESIS FROM ARYLCYCLOPROPANES

3,3-Biarylpropylamines represent a class of bioactive compounds in medicinal chemistry, encompassing numerous pharmacologically relevant structures such as Tolderodine, Fendiline, and Desfesoterodine. We report a concise and efficient synthetic approach to this scaffold via strain-release functionalization of aryl cyclopropanes through two complementary strategies. A copper-catalysed 1,3-aminoarylation and a photocatalyzed 1,3-aminochlorination of arylcyclopropanes, which can be combined with a Friedel–Crafts-type benzylation of arenes in a two-step, one-pot sequence and a were developed to access diverse 3,3-biarylpropylamine derivatives. Furthermore, this study has been subject of a data collection campaign, to obtain a dataset of labelled videos. The dataset has been used in the training of a multimodal model that aims to perform action recognition and hand-free workflow annotation in an electronic laboratory notebook.