Figure S1. Semi-preparative radio-HPLC purification of [18F]WC-DZ-F (retention time: 11 min). HPLC condition: Column: Agilent SB-18250 × 9.4 mm, 5 μm; mobile phase: 17% MeCN/83% water/0.1% TFA; flow rate: 4 mL/min; UV: 250 nm. After the collection of [18F]WC-DZ-F, the column was rinsed with 80% MeCN/20% water/0.1% TFA.

Figure S2. Analytical radio-HPLC of [18F]WC-DZ-F. HPLC condition: Column: Altima C18 250 × 4.6 mm, 10 μm; mobile phase: 18% MeCN/82% water/0.1% TFA; flow rate: 2 mL/min; UV: 250 nm. Note: The impurities eluting ahead of [18F]WC-DZ-F were not completed removed by semi-preparative radio-HPLC under the above condition as shown in Figure S1.

Figure S3. Typical analytical radio-HPLC of copper-mediated radiofluorination of (4-formylphenyl)boronic acid (#1 injection) and 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzaldehyde (#2 injection) (Blue: UV/Red: Radioactivity).

Figure S4. Typical analytical radio-HPLC of copper-mediated radiofluorination of 3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzaldehyde (Blue: UV/Red: Radioactivity).

Figure S5. Typical analytical radio-HPLC of copper-mediated radiofluorination of 2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzaldehyde (Blue: UV/Red: Radioactivity).

Figure S6. Typical analytical radio-HPLC of copper-mediated radiofluorination of (4-methoxyphenyl)boronic acid (Blue: UV/Red: Radioactivity).

Figure S7. Typical analytical radio-HPLC of copper-mediated radiofluorination of (4-[trifluoromethyl]phenyl)boronic acid (Blue: UV/Red: Radioactivity).

Figure S8. Typical analytical radio-HPLC of copper-mediated radiofluorination of (4-fluorophenyl)boronic acid (Blue: UV/Red: Radioactivity).

Figure S9. Typical analytical radio-HPLC of copper-mediated radiofluorination of phenylboronic acid (Blue: UV/Red: Radioactivity).

Figure S10. Typical analytical radio-HPLC of copper-mediated radiofluorination of ethyl 2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoate (Blue: UV/Red: Radioactivity).

Figure S11. Typical analytical radio-HPLC of copper-mediated radiofluorination of tert-butyl 3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoate (a) and after deprotection (b) (Blue: UV/Red: Radioactivity). HPLC condition: Column: Altima C18 250 × 4.6 mm, 10 μm; mobile phase: gradient from 60% MeCN/40% water/0.1% TFA at 0 min to 80% MeCN/20% water/0.1% TFA at 10 min; flow rate: 2 mL/min; UV: 254 nm.

Figure S12. Semi-preparative radio-HPLC of copper-mediated radioiodination of [124I]KX-1 (Black: UV/Red: radioactivity). HPLC condition: Column: Agilent SB-18250 × 9.4 mm, 5 μm; mobile phase: 19% MeCN/81% water/0.1% TFA; flow rate: 4 mL/min; UV: 250 nm. After the collection of [124I]KX-1, the column was rinsed with 80% MeCN/20% water/0.1% TFA. [124I]KX-1 was collected at 30.2-32.5 min.