Currently, only a few 18 F-radiolabeling methods were conducted in aqueous media, with non-macroelement fluoride acceptors and stringent conditions required. Herein, we describe a one-step non-solvent-biased, room-temperature-driven 18 F-radiolabeling methodology based on organophosphine fluoride acceptors. The high water tolerance for this isotope-exchange-based 18 F-labeling method is attributed to the kinetic and thermodynamic preference of F/F over the OH/F substitution based on computational calculations and experimental validation. Compact [ 18/19 F]di- tert -butyl-organofluorophosphine and its derivatives used as 18 F-labeling synthons exhibit excellent stability in vivo. The synthons are further conjugated to several biomolecular ligands such as c(RGDyk) and human serum albumin. The one-step labeled biomolecular tracers demonstrate intrinsic target imaging ability and negligible defluorination in vivo. The current method thus offers a facile and efficient 18 F-radiolabeling pathway, enabling further widespread application of 18 F.

Although photoacoustic imaging (PAI) in the second near-infrared (NIR-II) region (1.0–1.7 μm) is admired for deeper penetration and higher contrast, few organic NIR-II absorbers are available as exogenous contrast agents in vivo. A1094 belongs to the very few ∼1.1 μm absorbing croconaine dyes that have superior extinction coefficient and tend to form irregular aggregation. In this study, shape-controlled A1094@DSPE-PEG2000 micelles with a J-aggregate core with remarkable 1.2–1.3 μm absorption are fabricated as biocompatible organic agents. Excellent capabilities in photothermal conversion, photostability, and PAI are found in in vitro studies. In vivo PAI of inguinal lymph nodes and in situ glioma pre- and post-resection, all demonstrate high lymph/tumor-targeting efficiency. An ∼4.54 mm deep brain lesion is imaged at 1200 nm with minimized background and increased contrast compared to 970 nm. Overall, we achieved significant bathochromic shift of organic absorbers and expanded their PAI application to the long-wavelength end of the NIR-IIa region.

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