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The inverse electron demand Diels-Alder cycloaddition with carbon-11 and fluorine-18: A gateway to pretargeted imaging across the blood-brain barrier

期刊: JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2023; 66 (9)

There is increased focus on developing tools to image large biomolecules, such as antibodies, within the brain using positron emission tomography (PET......

Mild and selective hydrogen-deuterium exchange for aromatic hydrogen of amines

期刊: JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2023; 66 (10)

The direct electrophilic deuteration of the aromatic moiety in aromatic and aralkyl amines is reported. The acid-catalyzed deuteration is facilitated ......

Small-scale two-dimensional liquid chromatography for a preparative re-purification of a highly labile tritium-labeled compound

期刊: JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2023; 66 (7-8)

Tritium-labeled compounds are generally less stable than their non-labeled counterparts. This requires storage at low temperatures, a constant workflo......

Development of an economical method to synthesize O-(2-[18F]fluoroethyl)-L-tyrosine (18FFET)

期刊: JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2023; 66 (11)

Positron emission tomography (PET) using O-(2-[F-18]fluoroethyl)-L-tyrosine ([F-18]FET) has shown great success in differentiating tumor recurrence fr......

Photocatalyzed radiosynthesis of 11C-phenylacetic acids

期刊: JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2023; ()

Fast and straightforward incorporation of radionuclides into pharmaceutically relevant molecules is one of the main barriers to preclinical and clinic......

Peptides for trans-blood-brain barrier delivery

期刊: JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2023; 66 (9)

Trans-blood-brain barrier (BBB) delivery of therapeutic and diagnostic agents is a major challenge in the development of central nervous system (CNS) ......

Synthesis of trifold-labeled versatile reagent [3,5-13C2,4-15 N]4-phenyl-1,2,4-triazoline-3,5-dione

期刊: JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2023; 66 (14)

Triazolinediones are an important class of derivatization agents that have found application in various research disciplines. Their unique reactivity ......

Improved protocol for the radiosynthesis of [18F]FTC-146: A potent and selective sigma-1 receptor radioligand

期刊: JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2023; 66 (3)

[F-18]FTC-146 was introduced as a very potent and selective sigma-1 receptor radioligand, which has shown promising application as an imaging agent fo......

[11C]CO2 BOP fixation with amines to access 11C-labeled ureas for PET imaging

期刊: JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2023; ()

Carbon-11 (C-11) is a widely used radionuclide for positron emission tomography (PET) owing to the omnipresence of carbon atoms in organic molecules. ......

Benzylic deuteration of alkylnitroaromatics via amine-base catalysed exchange with deuterium oxide

期刊: JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2023; 66 (1)

This paper describes the deuterium-labelling of alkylnitroaromatics by base-catalysed exchange with deuterium oxide. As the alkyl protons alpha to the......

Synthesis and analysis of isotopically stable labeled nitrosamines as mass spectrometry standards for drug impurity quality control

期刊: JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2023; 66 (2)

We describe a simple and easy pathway to synthesize nitrosamine mass spectrometry standards in good to moderate yields. N-alkylation of Boc-protected ......

Synthesis and preclinical evaluation of a selective MET kinase positron emission tomography tracer

期刊: JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2023; 66 (14)

The tyrosine kinase MET (hepatocyte growth factor receptor) is activated or mutated in a wide range of cancers and is often correlated with a poor pro......

Strategies for designing novel positron emission tomography (PET) radiotracers to cross the blood-brain barrier

期刊: JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2023; 66 (9)

Positron emission tomography (PET) is a powerful tool for imaging biological processes in the central nervous system (CNS). Designing PET radiotracers......

Development of a high-performance liquid chromatography method for rapid radiochemical purity measurement of [18F]PSMA-1007, a PET radiopharmaceutical for detection of prostate cancer

期刊: JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2023; 66 (3)

Since first becoming commercially available in 2018, the PET radiopharmaceutical [F-18]PSMA-1007 has been used widely for the diagnosis and staging of......

Synthesis and radiolabeling of a polar [125I]I-1,2,4,5-tetrazine

期刊: JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2023; 66 (1)

Pretargeting imaging has gained a lot of prominence, due to its excellent bioorthogonality and improved imaging contrast compared to conventional imag......

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