Arylated cyclobutanes were accessed by a versatile palladium-catalyzed secondary C(sp3)−H activation, exploiting chelation assistance by modular triazoles. The C−H arylation led to cyclobutane natural product derivatives in a highly regioselective fashion, setting the stage for the easy access to novel fluorogenic boron-dipyrrin (BODIPY)-labeled probes for live-cell imaging. © 2019 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim