Efficient <sup>11</sup>C‑Carbonylation of Isolated
Aryl Palladium Complexes for PET: Application to Challenging Radiopharmaceutical
Synthesis
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Abstract
We
describe the successful implementation of palladium-aryl oxidative
addition complexes as stoichiometric reagents in carbonylation reactions
with <sup>11</sup>CO to produce structurally challenging, pharmaceutically
relevant compounds. This method enables the first <sup>11</sup>C-carbonyl
labeling of an approved PET tracer, [<sup>11</sup>C]raclopride, for
the dopamine D2/D3 receptor by carbonylation with excellent radiochemical
purity and yield. Two other molecules, [<sup>11</sup>C]olaparib and
[<sup>11</sup>C]JNJ 31020028, were efficiently labeled in this manner.
The technique distinguishes itself from existing methods by the markedly
improved purity profiles of the tracer molecules produced and provides
access to complex structures in synthetically useful yields, hereby
offering a viable alternative to other <sup>11</sup>C-labeling strategies