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Table 1 The table of optimization for step 2 from [18F]15 to [18F]1

From: Synthesis and preclinical evaluation of a novel fluorine-18 labeled small-molecule PET radiotracer for imaging of CXCR3 receptor in mouse models of atherosclerosis

Entry

Solvent

Additive

Temp

RCC (%)a

1

MeOH

HOAc

50

 < 3

2

MeOH

None

50

–

3

DMF

HOAc

50

5 ± 3

4

DMF

HOAc

110

12 ± 5

5

DMF

None

110

 < 5

6

DMSO

None

110

11 ± 5

7

DMSO

HOAc

110

36 ± 4

  1. Conditions: [18F]15 (740–2220 MBq), 9 (5 ± 0.5 mg), NaBH3CN (11 ± 1 mg), HOAc (10 μL), 20 min
  2. aBased on radio-TLC (0.1% Et3N, 10% MeOH in DCM, Rf 0.3)