Daniel Pla

Terpene‐derived alkaloids show a variety of biological activities, including antioxidant, anti‐inflammatory, antimicrobial and cytotoxicity effects. In this work, homologated monoterpene amines have been prepared via a rhodium‐catalyzed hydroaminomethylation of biomass‐based alkenes, such as ( R )‐limonene, linalool, myrcene and camphene, in combination with secondary amines of aliphatic and aromatic nature, namely morpholine and N ‐methylaniline, leading to highly chemo‐ and regioselective processes. The as‐prepared amines were obtained in 50–99 % overall yields, and in vitro tested on a human colon cancer cell line (HCT‐116) to evaluate their cytotoxic potential. The lead compound of the series ( 3 a ) showed cytotoxicity in the micromolar range (IC50 52.46 μM) via the induction of cell death by apoptosis, paving the way towards further structure‐activity relationship studies.