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High‐Yielding, Two‐Step 18 F Labeling Strategy for 18 F‐PARP1 Inhibitors
Author(s) -
Keliher Edmund J.,
Reiner Thomas,
Turetsky Anna,
Hilderbrand Scott A.,
Weissleder Ralph
Publication year - 2011
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201000426
Subject(s) - bioorthogonal chemistry , cycloaddition , positron emission tomography , pet imaging , computer science , chemistry , yield (engineering) , small molecule , combinatorial chemistry , radiochemistry , information retrieval , physics , click chemistry , nuclear medicine , biochemistry , medicine , catalysis , thermodynamics
Speedy and easy! An 18 F‐labeled PARP1 imaging agent, based on AZD2281, was prepared via an inverse electron demand Diels–Alder cycloaddition in high radiochemical yield for positron emission tomography (PET) imaging. This strain‐promoted ‘bioorthogonal’ reaction is envisioned to be a widely applicable 18 F‐labeling strategy for repeat and on‐demand synthesis of small molecules for PET imaging.