Radiosynthesis of 11C6-OH-BTA-1 in Different Media and Confirmation of Reaction By-products / 핵의학분자영상
Nuclear Medicine and Molecular Imaging
; : 241-246, 2007.
Article
ي Ko
| WPRIM
| ID: wpr-162720
المكتبة المسؤولة:
WPRO
ABSTRACT
PURPOSE:
[11C]6-OH-BTA-1 ([N-methyl-11C]2-(4'-methylaminophenyl)-6-hydroxybenzothiazole, 1), a -amyloid imaging agent for the diagnosis of Alzheimer's disease in PET, can be labeled with higher yield by a simple loop method. During the synthesis of [11C]1, we found the formation of by-products in various solvents, e.g., methylethylketone (MEK), cyclohexanone (CHO), diethylketone (DEK), and dimethylformamide (DMF). MATERIALS ANDMETHODS:
In Automated radiosynthesis module, 1 mg of 4-aminophenyl-6-hydroxybenzothiazole (4) in 100 l of each solvent was reacted with [11C]methyl triflate in HPLC loop at room temperature (RT). The reaction mixture was separated by semi-preparative HPLC. Aliquots eluted at 14.4, 16.3 and 17.6 min were collected and analyzed by analytical HPLC and LC/MS spectrometer.RESULTS:
The labeling efficiencies of [11C]1 were 86.0+/-5.5%, 59.7+/-2.4%, 29.9+/-1.8%, and 7.6+/-0.5% in MEK, CHO, DEK and DMF, respectively. The LC/MS spectra of three products eluted at 14.4, 16.3 and 17.6 mins showed m/z peaks at 257.3 (M+1), 257.3 (M+1) and 271.3 (M+1), respectively, indicating their structures as 1, 2-(4'-aminophenyl)-6-methoxybenzothiazole (2) and by-product (3), respectively. Ratios of labeling efficiencies for the three products ([11C]1[11C]2[11C]3) were 86.0+/-5.5%5.0+/-3.4%1.5+/-1.3% in MEK, 59.7+/-2.4%4.7+/-3.2%1.3+/-0.5% in CHO, 9.9+/-1.8%2.0+/-0.7%0.3+/-0.1% in DEK and 7.6+/-0.5%0.0%0.0% in DMF, respectively.CONCLUSION:
The labeling efficiency of [11C]1 was the highest when MEK was used as a reaction solvent. As results of mass spectrometry, 1 and 2 were conformed. 3 was presumed.Key words
النص الكامل:
1
الفهرس:
WPRIM
الموضوع الرئيسي:
Solvents
/
Mass Spectrometry
/
Chromatography, High Pressure Liquid
/
Diagnosis
/
Dimethylformamide
/
Alzheimer Disease
نوع الدراسة:
Diagnostic_studies
اللغة:
Ko
مجلة:
Nuclear Medicine and Molecular Imaging
السنة:
2007
نوع:
Article