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Automated preparation of 2‐[ 18 F]fluoropropionate labeled peptides using a flexible, multi‐stage synthesis platform (iPHASE Flexlab)
Author(s) -
Haskali Mohammad B.,
Roselt Peter D.,
Hicks Rodney J.,
Hutton Craig A.
Publication year - 2018
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3580
Subject(s) - chemistry , radiochemistry , stage (stratigraphy) , combinatorial chemistry , chromatography , paleontology , biology
Radiolabelled peptides are vital tools used in positron emission tomography imaging for the diagnosis of disease, drug discovery, and biomedical research. Peptides are typically labeled through conjugation to a radiolabelled prosthetic group, which usually necessitates complex, multi‐step procedures, especially for fluorine‐18 labeled peptides. Herein, we describe the automated synthesis and formulation of 2‐[ 18 F]fluoropropionate labeled RGD‐peptides through use of the iPHASE Flexlab as an effective dual‐stage radiochemical synthesis module. The fully automated preparation of the monomeric RGD‐peptides, [ 18 F]FP‐GalactoRGD and [ 18 F]FP‐c(RGDy(SO 3 )K), was accomplished in under 90 minutes with n.d.c. radiochemical yields ca. 7% from fluoride. Similarly, the automated preparation of the dimeric RGD‐peptides, [ 18 F]F‐PRGD 2 and [ 18 F]FP‐E(RGDy(SO 3 )K) 2 , was accomplished in under 105 minutes with n.d.c. yields ca. 4% from fluoride.