Synthesis of [18F]FPPRGD2

Radiochemical Syntheses: Radiopharmaceuticals for Positron Emission Tomography

Volumn 1, Issue , 2012, Pages 51-60

  Liu, Shuanglong ^a   Chin, Frederick T ^a   Cheng, Zhen ^a   Chen, Xiaoyuan ^a,b  

^a STANFORD UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b NATIONAL INSTITUTE OF BIOMEDICAL IMAGING AND BIOENGINEERING   (United States)

Author keywords

Purification and formulation of 18F FPPRGD2; QC data for three repeat runs of 18F FPPRGD2; Synthesis of 18F FPPRGD2

Indexed keywords

EID: 84886142860     PISSN: None     EISSN: None     Source Type: Book    
DOI: 10.1002/9781118140345.ch6     Document Type: Chapter

References (23)

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9. 2O >95% isotopic enrichment was purchased from Rotem Industries Ltd., Israel, and used as received.
10. GEMS silver high yield [18F]fluoride target.
11. GE Healthcare, USA.
12. 3 cartridges (catalog No. 731876) were purchased from Macharey-Nagel, Germany, and conditioned with 1 mL ethanol and 1 mL water before use and dried over air flow.
13. Potassium carbonate was purchased from Aldrich (catalog No. 367877) and used as received. Kryptofix-[2.2.2] was purchased from Aldrich and (catalog No. 291110) and used as received. Acetonitrile was purchased from Aldrich (catalog No. 271004) and used as received. Sterile water was purchased from Hospipra, Inc., USA, (catalog No. NDC 0409-4887-10) and used as received.
14. The semipreparative reversed-phase high performance liquid chromatography (RP-HPLC) using a Vydac protein and peptide column (218TP510; 5 μm, 250 × 10 mm) was performed on Dionex 680 pump with KANUR UV detector K-2001. With a flow rate of 5 mL/min, the mobile phase was changed from 95% solvent A [0.1% trifluoroacetic acid (TFA) in water] and 5% B [0.1% TFA in acetonitrile (MeCN)] (0-2 min) to 35% solvent A and 65% solvent B at 32 min.
15. C-18 Sep-Pak cartridges were purchased from Waters, USA, (part no. WAT020515) and conditioned with 5 mL ethanol and 10 mL sterile water before use.
16. Sodium sulfate cartridges were purchased from Varian, USA, (part No. WAT054265) and used without any conditioning.
17. PRGD2 was purchased from Peptides International, USA (catalog No. PCS-37458-PI) and used as received.
18. The semipreparative reversed-phase high performance liquid chromatography (RP-HPLC) using Phenomenex column (Gemini, 5 μm, C18, 250 × 10 mm) with the flow rate at 7.5 mL/min was performed on Dionex Ultimate 3000 chromatography system with a UVD 340U absorbance detector. The mobile phase was started at 90% solvent A and 10% solvent B (0-2 min) and changed to 86.5% solvent A and 13.5% solvent B at 20 min, was kept at this percentage for 5 min, and then again gradually changed to 70% solvent A and 30% solvent B in 20 min.
19. U. S. Pharmacopeia <823> radiopharmaceuticals for Positron Emission Tomography Compounding, USP 32-NF 27. 2009.
20. 23, calculated molecular weight, 1613.8).
21. Radioactivity measurements were carried out with a CRC-15PET dose calibrator (Capintec Inc., USA), which was calibrated daily using Cs-137 (Bench/mark, USA) and Co-57 source (Isotope products laboratories, USA).
22. U. S. Pharmacopeia <85> Bacterial Endotoxins Test. USP 32-NF 27. 2009.
23. U.S. Pharmacopeia <71> Sterility Tests. USP 32-NF 27. 2009.