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An efficient Cu(II)-catalyzed, C–H alkylation of BODIPY with a variety of alkyl diacyl peroxides has been developed for the first time, providing a late-stage and straightforward method for controllable synthesis of monoalkylated and dialkylated BODIPYs via a radical process that otherwise is difficult to obtain by literature methods. This chemo- and site-selective transformation will allow for the introduction of a variety of functionalities on the BODIPY core for highly versatile tethering to receptors and to other molecules of interest.

Graphical abstract: Development of BODIPY dyes with versatile functional groups at 3,5-positions from diacyl peroxides via Cu(ii)-catalyzed radical alkylation

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