Please use this identifier to cite or link to this item: https://apo.ansto.gov.au/dspace/handle/10238/9213
Title: Synthesis and radiosynthesis of a novel PET fluorobenzyl piperazine for melanoma tumour imaging; [18F]MEL054
Authors: Taylor, SR
Roberts, MR
Wyatt, NA
Pham, TQ
Stark, D
Bourdier, T
Roselt, P
Katsifis, A
Greguric, I
Keywords: Fluorine 18
Radiochemistry
Piperazines
High-performance liquid chromatography
Melanin
Neoplasms
Alkylation
Issue Date: 18-Feb-2012
Publisher: CSIRO publishing
Citation: Taylor, 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/CH12489
Abstract: 2-{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.
Gov't Doc #: 8883
URI: https://doi.org/10.1071/CH12489
http://apo.ansto.gov.au/dspace/handle/10238/9213
ISSN: 0004-9425
Appears in Collections:Journal Articles

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