Automated radiosynthesis of the Pittsburg compound-B using a commercial synthesizer

Nuclear Medicine Communications

Volumn 29, Issue 10, 2008, Pages 920-926

  Verdurand, Mathieu ^a,b   Bort, Guillaume ^a,b   Tadino, Vincent ^a,b   Bonnefoi, Fréderic ^a,b   Le Bars, Didier ^a,b   Zimmer, Luc ^a,b  

^a UNIVERSITÉ LYON 1   (France)

^b Bioscan Inc   (United States)

Author keywords

Alzheimer; Automated synthesis; Positron emission tomography

Indexed keywords

2 (4' AMINOPHENYL) 6 HYDROXYBENZOTHIAZOLE; AMYLOID; BENZOTHIAZOLE DERIVATIVE; CARBON 11; METHYL IODIDE; NITROGEN; PITTSBURG COMPOUND B C 11; TRACER; TRIFLUOROMETHANESULFONIC ACID; UNCLASSIFIED DRUG; CARBON; N METHYL 2 (4' METHYLAMINOPHENYL) 6 HYDROXYBENZOTHIAZOLE; N-METHYL-2-(4'-METHYLAMINOPHENYL)-6-HYDROXYBENZOTHIAZOLE; RADIOPHARMACEUTICAL AGENT;

ALZHEIMER DISEASE; ARTICLE; AUTOMATED RADIOSYNTHESIS; DRUG STRUCTURE; DRUG SYNTHESIS; EQUIPMENT DESIGN; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; ISOTOPE LABELING; METHYLATION; POSITRON EMISSION TOMOGRAPHY; VALIDATION PROCESS; SYNTHESIS;

BENZOTHIAZOLES; CARBON RADIOISOTOPES; RADIOPHARMACEUTICALS;

EID: 58749111447     PISSN: 01433636     EISSN: 14735628     Source Type: Journal    
DOI: 10.1097/MNM.0b013e328304e0e1     Document Type: Article

References (19)

1. Mathis CA, Bacskai BJ, Stephen T, Kajdasz ST, Mc Lellan ME, Frosch MP, et al. A lipophilic thioflavin-T derivative for positron emission tomography (PET) imaging of amyloid in brain. Bioorg Med Chem Lett 2002; 12:295-298.
2. Klunk WE, Wang Y, Huang GF, Debnath ML, Holt DP, Mathis CA. Uncharged thioflavine-T derivatives bind to amyloid-beta protein with high affinity and readily enters the brain. Life Sci 2001; 69:1471-1484.
3. Klunk WE, Wang Y, Huang GF, Debnath ML, Holt DP, Shao L, et al. The binding of 2-(4′methylaminophenyl)benzothiazole to post-mortem brain homogenates is dominated by the amyloid component. J Neurosci 2003; 23:2086-2092.
4. 11C-labelled 6-substituted 2-arylbenzothiazoles as amyloid imaging agents. J Med Chem 2003; 46:2740-2754.
5. Klunk WE, Engler E, Nordberg A, Wang Y, Blomqvist G, Holt DP, et al. Imaging brain amyloid in Alzheimer's disease with Pittsburgh compound-B. Ann Neurol 2004; 55:306-319.
6. 11C]methyl triflate for β-amyloid imaging in Alzheimer's disease with PET. Appl Radiat Isotop 2005; 62:591-595.
7. 11C]methyl triflate. Appl Radiat Isotop 1992; 43:1383-1385.
8. 11C]-6-OH-BTA-1). J Label Compd Radiopharm 2004; 47:679-682.
9. 11C]-iodomethane: a remarkably simple captive solvent method. Nucl Med Biol 2000; 27:529-532.
10. Ono M, Wilson A, Nobrega J, Westaway D, Verhoeff P, Zhuang ZP, et al. 11C-labeled stilbene derivatives as Abeta-aggregate-specific PET imaging agents for Alzheimer's disease. Nucl Med Biol 2003; 30:565-571.
11. 11C]acetate. Appl Radiat Isotop 1997; 48:1117-1120.
12. 11C]-carboxylation of an immobilized Grignard reagent. J Label Compd Radiopharm 1996; 38:941-953.
13. Dannals RF, Langstrom B. A simple one-pot apparatus for the production of carbon-11 labeled methyl iodide. J Nucl Med 1985; 26:126.
14. 11C]methyl triflate. Int J Appl Radiat Isot 1992; 1992:1383-1385.
15. Lemaire C, Plénevaux A, Aerts J, Del Fiore G, Brihaye C, Le Bars D, et al. Solid phase extraction - an alternative to the use of rotary evaporators for solvent removal in the rapid formulation of PET radiopharmaceuticals. J Label Compd Radiopharm 1999; 42:63-75.
16. 11C]methyl iodide. Int Appl Radiat Isot 1987; 38:601-604.
17. Mock BH, Mulholland GK, Vavrek MT. Convenient gas phase bromination of [11C]methane and production of [11C]methyl triflate. Nucl Med Biol 1999; 26:467-471.
18. 11C]methyl triflate. Appl Radiat Isotop 2001; 55:17-22.
19. Mock BH, Zheng QH, Degrado TR. Avoid DMF when labeling with 11C-methyl triflate. J Label Compd Radiopharm 2007; 50:S197.