Abstract:
:In the last few years click chemistry reactions, and in particular copper-catalyzed cycloadditions have been used extensively for the preparation of new bioconjugated molecules such as (18)F-radiolabeled radiopharmaceuticals for positron emission tomography (PET). This study is focused on the synthesis of the Siemens imaging biomarker [(18)F]RGD-K5. This cyclic peptide contains an amino acid sequence which is a well known binding motif for integrin αvβ3 involved in cellular adhesion to the extracellular matrix. We developed an improved "click" chemistry method using Cu(I)-Monophos as catalyst to conjugate [(18)F]fluoropentyne to the RGD-azide precursor yielding [(18)F]RGD-K5. A comparison is made with the registered Siemens method with respect to synthesis, purification and quality control. [(18)F]RGD-K5 was obtained after 75 min overall synthesis time with an overall radiochemical yield of 35% (EOB). The radiochemical purity was >98% and the specific radioactivity was 100-200 GBq/μmol at the EOS.
journal_name
Nucl Med Bioljournal_title
Nuclear medicine and biologyauthors
Mirfeizi L,Walsh J,Kolb H,Campbell-Verduyn L,Dierckx RA,Feringa BL,Elsinga PH,de Groot T,Sannen I,Bormans G,Celen Sdoi
10.1016/j.nucmedbio.2013.04.003subject
Has Abstractpub_date
2013-07-01 00:00:00pages
710-6issue
5eissn
0969-8051issn
1872-9614pii
S0969-8051(13)00076-0journal_volume
40pub_type
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更新日期:2016-01-01 00:00:00