Synthesis optimization of 2-(4-N-[11C]methylaminophenyl)-6-hydroxybenzothiazole ([11C]PIB), β-amyloid PET imaging tracer for Alzheimer's disease diagnosis. (November 2015)

• Record Type: Journal Article
• Authors: Coliva, A.; Monterisi, C.; Apollaro, A.; Gatti, D.; Penso, M.; Gianolli, L.; Perani, D.; Gilardi, M.C.; Carpinelli, A.
• Is Part Of: Applied radiation and isotopes. Volume 105(2015:Nov.)
• Page Start: 66
• Page End: 71
• Publication Date: 2015-11
• Subjects: Cyclotron -- Alzheimer's disease -- [11C]MeOTf -- [11C]PIB -- β-amyloid; Radiology -- Periodicals; Radiation -- Industrial applications -- Periodicals; Nuclear chemistry -- Periodicals; Internet resource; Periodical; 660.298
• DOI: 10.1016/j.apradiso.2015.07.003
• Languages: English
• ISSNs: 0969-8043

Abstract

Abstract: [11C]PIB is the most used amyloid plaques-specific positron-emitting radiotracers. The radiosynthesis of this compound, carried out by methylation of its precursor with [11C]methyl triflate in 2-butanone, has been improved optimizing the initial concentration and the purification method. Two HPLC methods were compared: good radiochemical yields, specific activities, and chemical purity above 98% were achieved by using as eluant acetonitrile/citrate and formulation in 10% ethanol. Highlights: Good yields and specific activity of [11C]PIB were obtained by reaction parameters optimization. Improvement of the HPLC purification. Quality parameters and drug formulation allows a readily application in clinic.