| 1. |
- Andersen, Thomas L., et al.
(författare)
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Application of Methyl Bisphosphine-Ligated Palladium Complexes for Low Pressure N-C-11-Acetylation of Peptides
- 2017
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Ingår i: Angewandte Chemie International Edition. - : Wiley. - 1433-7851 .- 1521-3773. ; 56:16, s. 4549-4553
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Tidskriftsartikel (refereegranskat)abstract
- A mild and effective method is described for C-11-labeling of peptides selectively at the N-terminal nitrogen or at internal lysine positions. The presented method relies on the use of specific biphosphine palladium-methyl complexes and their high reactivity towards amino-carbonylation of amine groups in the presence [C-11] carbon monoxide. The protocol facilitates the production of native N-C-11-acetylated peptides, without any structural modifications and has been applied to a selection of bioactive peptides.
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| 2. |
- Andersen, Thomas L., et al.
(författare)
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Efficient C-11-Carbonylation of Isolated Aryl Palladium Complexes for PET : Application to Challenging Radiopharmaceutical Synthesis
- 2015
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Ingår i: Journal of the American Chemical Society. - : American Chemical Society (ACS). - 0002-7863 .- 1520-5126. ; 137:4, s. 1548-1555
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Tidskriftsartikel (refereegranskat)abstract
- 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.
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| 3. |
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| 4. |
- Nordeman, Patrik, et al.
(författare)
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Rapid and Efficient Conversion of (CO2)-C-11 to (CO)-C-11 through Silacarboxylic Acids : Applications in Pd-Mediated Carbonylations
- 2015
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Ingår i: Chemistry - A European Journal. - : Wiley. - 0947-6539 .- 1521-3765. ; 21:49, s. 17601-17604
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Tidskriftsartikel (refereegranskat)abstract
- Herein, we present a new rapid, efficient, and low-cost radiosynthetic protocol for the conversion of (CO2)-C-11 to (CO)-C-11 and its subsequent application in Pd-mediated reactions of importance for PET applications. This room-temperature methodology, using readily available chemical reagents, is carried out in simple glass vials, thus eliminating the need for expensive and specialized high-temperature equipment to access (CO)-C-11. With this fast and near-quantitative conversion of (CO2)-C-11 into (CO)-C-11, aryl and heteroaryl iodides were easily converted into a broad selection of biologically active amides in radiochemical yields ranging from 29-84 %.
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