Issue Information
No abstract is available for this article. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - October 3, 2023 Category: Biochemistry Tags: ISSUE INFORMATION Source Type: research

Total synthesis of [13C2] ‐labeled phytosiderophores of the mugineic and avenic acid families
In this work, we report the modular synthesis of all naturally occurring members from the mugineic acid and avenic acid family in13C2-labeled form. The syntheses commence from available13C2-bromoacetic acid and13C2-glycine delivering labeled building blocks13C2-l-allylglycine and a related hydroxylated derivative, both potentially valuable for other synthetic routes toward labeled (natural) products. We, herein, report the synthesis of13C2-labeled natural products from the mugineic acid and avenic acid family. These phytosiderophores ( “plant iron carriers”) are built up from non-proteinogenic amino acids and play a ke...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - October 2, 2023 Category: Biochemistry Authors: Nicolas Kratena, Markus Draskovits, Nina Biedermann, Eva Oburger, Christian Stanetty Tags: RESEARCH ARTICLE Source Type: research

A practical protocol for large ‐scale copper‐mediated radioiodination of organoboronic precursors: Radiosynthesis of [123I]KX‐1 for Auger radiotherapy
Neutralization of the strong basic solution of [123]NaI/NaOH with an acid (pyridiniump-toluenesulfonate) promotes the radiosynthesis of [123I]KX-1 on large-scale via copper-mediated radioiodination (CMRI) of the organoboronic precursor in high radiochemical yield, high radiochemical purity, and high molar activity. This strategy should be applicable to the radiosynthesis of other radioiodine-labeled compounds via CMRI. Nucleophilic copper-mediated radioiodination (CMRI) of organoboronic precursors with radioiodides is a promising method of radioiodination. The previously reported CMRI has demonstrated its great potential a...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - September 22, 2023 Category: Biochemistry Authors: Dong Zhou, Wenhua Chu, Jinbin Xu Tags: NOTE Source Type: research

Stable isotope synthesis of glycine transporter 1 inhibitor Iclepertin (BI 425809) and its major metabolites
Iclepertin (BI 425809) is a potent and selective GlyT-1 inhibitor being developed for the treatment of schizophrenia. The detailed stable isotope synthesis of this drug candidate and its major metabolites is described. Stable isotope labeledIclepertin (BI 425809, 1) and its major metabolites are needed as internal standards in bioanalytical studies.BI 425809 consists of two main building blocks, 5-methylsulfonyl-2-[(1R)-2,2,2-trifluoro-1-methyl-ethoxy]benzoic acid (2) and 3-[(1R,5R)-3-azabicyclo[3.1.0]hexan-5-yl]-5-(trifluoromethyl)isoxazole (3) linked to each other via an amide bond. We used fluoro[13C6]benzene as the sta...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - September 21, 2023 Category: Biochemistry Authors: Bachir Latli, Matt J. Hrapchak, Maxim Chevliakov, Lalith P. Samankumara, Rogelio P. Frutos, Heewon Lee Tags: RESEARCH ARTICLE Source Type: research

Issue Information
No abstract is available for this article. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - September 11, 2023 Category: Biochemistry Tags: ISSUE INFORMATION Source Type: research

Preliminary PET imaging of [11C]evobrutinib in mouse models of colorectal cancer, SARS ‐CoV‐2, and lung damage: Radiosynthesis via base‐aided palladium‐NiXantphos‐mediated 11C‐carbonylation
In conclusion, [11C]evobrutinib was successfully synthesized by11C-carbonylation and based on our preliminary studies does not appear to be a promising BTK-targeted PET radiotracer in the rodent disease models studied herein. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - September 11, 2023 Category: Biochemistry Authors: Amanda J. Boyle, Anton Lindberg, Junchao Tong, Dongxu Zhai, Fang Liu, Neil Vasdev Tags: RESEARCH ARTICLE Source Type: research

[68Ga]Ga ‐PentixaFor: Development of a fully automated in hospital production on the Trasis miniAllinOne synthesizer
[68Ga]Ga-PentixaFor was conveniently prepared in sterile conditions, with the new fully automated and highly reproducible process we developed on the miniAiO ® synthesizer. The final product conforms with the European Pharmacopeia specifications. This automated production of [68Ga]Ga-PentixaFor and its availability allow to perform clinical studies in our hospital and to increase the access of patients to this new promising radiopharmaceutical. [68Ga]Ga-PentixaFor is a frequently used radiotracer to image the CXCR4/CXCL12 axis in various malignancies, infections, and cardiovascular diseases. To answer increasing clinical ...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - September 8, 2023 Category: Biochemistry Authors: Julien Costes, Kilian Casasagrande, Constance Dubegny, Juan Castillo, Jens Kaufman, Julien Masset, Charles Vriamont, Corentin Warnier, Alain Faivre ‐Chauvet, Judith Anna Delage Tags: RESEARCH ARTICLE Source Type: research