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. Author manuscript; available in PMC: 2023 Feb 2.
Published in final edited form as: Org Biomol Chem. 2022 Feb 2;20(5):1041–1052. doi: 10.1039/d1ob02225c

Table 1.

Optimization of 18F-radiolabeling conditions from ortho-nitro benzaldehyde 10 or 11. a

graphic file with name nihms-1782236-t0010.jpg
Entry 10 or 11 (mg) Additive (μL) T (°C) [18F]12 RCY (%)b
1 11 (4.5) none 150 0
2 11 (9.2) none 150 <5
3 10 (9.5) none 150 <5
4 11 (18.2) none 150 50 ± 5
5 10 (18.5) none 150 55 ± 8
6 10 (4.5) DABCO (10) 150 45 ± 13
7 10 (4.5) DBU (10) 150 30 ± 6
8 10 (4.5) TMEDA (10) 150 65 ± 10
9 10 (4.5) DIPEA (10) 150 43 ± 12
10 10 (4.5) TMEDA (10) 120 20 ± 5
11 10 (2.3) TMEDA (10) 150 60 ± 13
12 10 (1.2) TMEDA (10) 150 12 ± 3
13c 10 (4.5) TMEDA (30) 150 70 ± 16
a

[18F]KF/K222, K2CO3, DMSO (300 μL), 5 min.

b

RCY was determined based on radio-TLC (n = 3).

c

1 μL H2O added.

DABCO: 1, 4-diaza[2.2.2]bicyclooctane; DBU: 1,8-diazabicyclo[5.4.0]undec-7-ene; TMEDA: N, N, N′, N′-tetramethylethylenediamine; DIPEA: N,N-diisopropylethylamine.