Synthesis and radiosynthesis of a novel PET fluorobenzyl piperazine for melanoma tumour imaging; [18F]MEL054

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dc.contributor.authorTaylor, SRen_AU
dc.contributor.authorRoberts, MRen_AU
dc.contributor.authorWyatt, NAen_AU
dc.contributor.authorPham, TQen_AU
dc.contributor.authorStark, Den_AU
dc.contributor.authorBourdier, Ten_AU
dc.contributor.authorRoselt, Pen_AU
dc.contributor.authorKatsifis, Aen_AU
dc.contributor.authorGreguric, Ien_AU
dc.date.accessioned2020-03-24T01:19:28Zen_AU
dc.date.available2020-03-24T01:19:28Zen_AU
dc.date.issued2012-02-18en_AU
dc.description.abstract2-{2-[4-(4-[18F]-Fluorobenzyl)piperazin-1-yl]-2-oxoethyl}isoindolin-1-one ([18F]MEL054), is a new potent indolinone-based melanin binder designed to target melanotic tumours. [18F]MEL054 was prepared by an automated two-step radiosynthesis, comprising of the preparation of 4-[18F]fluorobenzaldehyde from 4-formyl-N,N,N-trimethylanilinium triflate, followed by reductive alkylation with 2-(2-oxo-2-piperazin-1-ylethyl)isoindolin-1-one. 4-[18F]Fluorobenzaldehyde was prepared on a GE TRACERlab FXFN module in 68 ± 8 % radiochemical yield (RCY, non-decay corrected), purified by a Sep-Pak Plus C18 cartridge and eluted into the reactor of an in-house modified Nuclear Interface [18F]FDG synthesis module for the subsequent reductive alkylation reaction. HPLC purification produced [18F]MEL054 in a collected RCY of 34 ± 9 % (non-decay corrected), the total preparation time (including Sep-Pak Plus C18 and HPLC purification) did not exceed 105 min. The radiochemical purity of [18F]MEL054 was greater than 99 % with a specific radioactivity of 71–119 GBq μmol–1 and [18F]MEL054 remained stable in saline solution (>98 %) after 3 h. © 2013 CSIRO.en_AU
dc.identifier.citationTaylor, S. R., Roberts, M. P., Wyatt, N. A., Pham, T. Q., Stark, D., Bourdier, T., Roselt, P., Katsifis, A., & Greguric, I. (2013). Synthesis and radiosynthesis of a novel PET Fluorobenzyl piperazine for melanoma tumour imaging; [18F] MEL054. Australian Journal of Chemistry, 66(4), 491-499. doi:10.1071/CH12489en_AU
dc.identifier.govdoc8883en_AU
dc.identifier.issn0004-9425en_AU
dc.identifier.issue4en_AU
dc.identifier.journaltitleAustralian Journal of Chemistryen_AU
dc.identifier.pagination491-499en_AU
dc.identifier.urihttps://doi.org/10.1071/CH12489en_AU
dc.identifier.urihttp://apo.ansto.gov.au/dspace/handle/10238/9213en_AU
dc.identifier.volume66en_AU
dc.language.isoenen_AU
dc.publisherCSIRO publishingen_AU
dc.subjectFluorine 18en_AU
dc.subjectRadiochemistryen_AU
dc.subjectPiperazinesen_AU
dc.subjectHigh-performance liquid chromatographyen_AU
dc.subjectMelaninen_AU
dc.subjectNeoplasmsen_AU
dc.subjectAlkylationen_AU
dc.titleSynthesis and radiosynthesis of a novel PET fluorobenzyl piperazine for melanoma tumour imaging; [18F]MEL054en_AU
dc.typeJournal Articleen_AU
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