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Efficient C-11-Carbonylation of Isolated Aryl Palladium Complexes for PET: Application to Challenging Radiopharmaceutical Synthesis
Uppsala universitet, Medicinska och farmaceutiska vetenskapsområdet, Farmaceutiska fakulteten, Institutionen för läkemedelskemi, Plattformen för preklinisk PET.
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2015 (engelsk)Inngår i: Journal of the American Chemical Society, ISSN 0002-7863, E-ISSN 1520-5126, Vol. 137, nr 4, s. 1548-1555Artikkel i tidsskrift (Fagfellevurdert) Published
Abstract [en]

We describe the successful implementation of palladium-aryl oxidative addition complexes as stoichiometric reagents in carbonylation reactions with (CO)-C-11 to produce structurally challenging, pharmaceutically relevant compounds. This method enables the first C-11-carbonyl labeling of an approved PET tracer, [C-11]raclopride, for the dopamine D2/D3 receptor by carbonylation with excellent radiochemical purity and yield. Two other molecules, [C-11]olaparib and [C-11]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 C-11-labeling strategies.

sted, utgiver, år, opplag, sider
2015. Vol. 137, nr 4, s. 1548-1555
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Identifikatorer
URN: urn:nbn:se:uu:diva-247393DOI: 10.1021/ja511441uISI: 000349138600029PubMedID: 25569730OAI: oai:DiVA.org:uu-247393DiVA, id: diva2:796826
Tilgjengelig fra: 2015-03-20 Laget: 2015-03-18 Sist oppdatert: 2018-01-11bibliografisk kontrollert

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