Journal of labelled compounds & radiopharmaceuticals最新文献_第9页

Photocatalyzed radiosynthesis of 11C-phenylacetic acids 11C-苯乙酸的光催化放射合成。

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2023-11-08 DOI: 10.1002/jlcr.4073

Maxime Munch, Braeden A. Mair, Myriam Adi, Benjamin H. Rotstein

引用次数: 0

Preparation and evaluation of radiolabeled acetaminosalol microspheres: A new potential selective radiotracer for ulcerative colitis early diagnosis 放射性标记乙酰氨基酚微球的制备和评价：一种新的潜在的选择性放射性示踪剂，用于溃疡性结肠炎的早期诊断。

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2023-11-07 DOI: 10.1002/jlcr.4070

O. A. El-Kawy, H. A. Shweeta, M. R. Abdelgawad

引用次数: 0

A simplified protocol for the automated production of 2-[18F]fluoro-3-[2-((S)-3-pyrrolinyl)methoxy]pyridine ([18F]nifene) on an IBA Synthera® module 在IBA Synthera®模块上自动生产2-[18F]氟-3-[2-（（S）-3-吡咯烷基）甲氧基]吡啶（[18F]niffee）的简化方案。

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2023-11-05 DOI: 10.1002/jlcr.4071

Mohammed Bhuiyan, Jeffrey Souris, Anna Kucharski, Richard Freifelder, Jogeshwar Mukherjee, Chin-Tu Chen

引用次数: 0

Site-specifically radiolabeled nanobodies for imaging blood-brain barrier penetration and targeting in the brain 位点特异性放射性标记的纳米体，用于对脑中血脑屏障的穿透和靶向进行成像。

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2023-10-24 DOI: 10.1002/jlcr.4069

Yingbo Li, Junfeng Wang

引用次数: 0

Synthesis and preclinical evaluation of a selective MET kinase positron emission tomography tracer 选择性MET激酶正电子发射断层扫描示踪剂的合成和临床前评估。

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2023-10-22 DOI: 10.1002/jlcr.4066

Vegard Torp Lien, Emily Hauge, Syed Nuruddin, Jo Klaveness, Dag Erlend Olberg

引用次数: 0

Total synthesis of [13C2]-labeled phytosiderophores of the mugineic and avenic acid families 木霉酸和燕麦酸家族[13C2]-标记的植物铁载体的全合成。

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2023-09-26 DOI: 10.1002/jlcr.4064

Nicolas Kratena, Markus Draskovits, Nina Biedermann, Eva Oburger, Christian Stanetty

{"title":"Total synthesis of [13C2]-labeled phytosiderophores of the mugineic and avenic acid families","authors":"Nicolas Kratena, Markus Draskovits, Nina Biedermann, Eva Oburger, Christian Stanetty","doi":"10.1002/jlcr.4064","DOIUrl":"10.1002/jlcr.4064","url":null,"abstract":"We, herein, report the synthesis of 13C2-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 key role in micronutrient uptake in gramineous plants. In this work, two central building blocks are prepared from labeled starting materials (13C2-bromoacetic acid, 13C2-glycine) and further employed in our recently reported divergent, branched synthetic strategy delivering eight isotopically labeled phytosiderophores. The required labeled building blocks (13C2-l-allylglycine and a related hydroxylated derivative) were prepared via enantioselective phase-transfer catalysis and enantio- and diastereoselective aldol condensation with a chiral auxiliary, respectively, both potentially valuable themselves for other synthetic routes toward labeled (natural) products.","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"66 13","pages":"428-434"},"PeriodicalIF":1.8,"publicationDate":"2023-09-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://analyticalsciencejournals.onlinelibrary.wiley.com/doi/epdf/10.1002/jlcr.4064","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41135766","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

A practical protocol for large-scale copper-mediated radioiodination of organoboronic precursors: Radiosynthesis of [123I]KX-1 for Auger radiotherapy 大规模铜介导的有机硼前体放射性碘化的实用方案：用于俄歇放射治疗的[123I]KX-1的放射合成。

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2023-09-21 DOI: 10.1002/jlcr.4065

Dong Zhou, Wenhua Chu, Jinbin Xu

{"title":"A practical protocol for large-scale copper-mediated radioiodination of organoboronic precursors: Radiosynthesis of [123I]KX-1 for Auger radiotherapy","authors":"Dong Zhou, Wenhua Chu, Jinbin Xu","doi":"10.1002/jlcr.4065","DOIUrl":"10.1002/jlcr.4065","url":null,"abstract":"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 and scope of labeling for the radiosynthesis of radioiodine-labeled compounds. However, the reported protocols (using a small amount/volume of radioactivity) are practically not reproducible in large-scale CMRI, in which the radioactivity was usually provided in a bulk alkaline solution. A large amount of water and a strong base are incompatible with CMRI. To overcome these issues in large-scale CMRI, we have developed a simple protocol for large-scale CMRI. The bulk water was removed under a flow of inert gas at 110°C, and the strong base (i.e., NaOH) was neutralized with an acid, pyridinium p-toluenesulfonate or p-toluenesulfonic acid. In the model reactions of [123I]KX-1, a PARP-1 radioligand for Auger radiotherapy, radiochemical conversions were significantly improved after neutralization of the base, and the addition of additional acids was tolerated and favorable for the reactions. Using this protocol, [123I]KX-1 was radiosynthesized from 20 mCi (0.74 GBq) of [123I]iodide in high radiochemical yields, high radiochemical purity, and high molar activity. This protocol should be applicable to the radiosynthesis of other compounds with radioiodine via CMRI.","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"66 13","pages":"435-439"},"PeriodicalIF":1.8,"publicationDate":"2023-09-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41148134","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Stable isotope synthesis of glycine transporter 1 inhibitor Iclepertin (BI 425809) and its major metabolites 甘氨酸转运蛋白1抑制剂Iclepertin（BI 425809）及其主要代谢产物的稳定同位素合成。

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2023-09-20 DOI: 10.1002/jlcr.4063

Bachir Latli, Matt J. Hrapchak, Maxim Chevliakov, Lalith P. Samankumara, Rogelio P. Frutos, Heewon Lee

{"title":"Stable isotope synthesis of glycine transporter 1 inhibitor Iclepertin (BI 425809) and its major metabolites","authors":"Bachir Latli, Matt J. Hrapchak, Maxim Chevliakov, Lalith P. Samankumara, Rogelio P. Frutos, Heewon Lee","doi":"10.1002/jlcr.4063","DOIUrl":"10.1002/jlcr.4063","url":null,"abstract":"Stable isotope labeled Iclepertin (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 starting material in the preparation of [13C6]-2. This intermediate was then employed to access carbon 13 labeled Iclepertin ([13C6]-1) and other metabolites. The major metabolite BI 761036 (6), which resulted from cytochrome P450 oxidation and amide hydrolysis of BI 425809, was prepared labeled with carbon 13 and nitrogen 15 via two synthetic routes. In the first route, diethyl [13C3]malonate, [13C]methyl iodide, and hydroxyl[15N]amine were used to provide [13C4,15N]-BI 761036 ([13C4,15N]-6a) in 13 steps in 6% overall yield, whereas in the second route, [13C3]propargyl alcohol, potassium [13C]cyanide, and [15N]ammonia were used to furnish [13C4,15N]-BI 761036 ([13C4,15N]-6b) in 11 steps in 1% overall yield. The detailed stable isotope synthesis of 1 and its major metabolites is described.","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"66 13","pages":"414-427"},"PeriodicalIF":1.8,"publicationDate":"2023-09-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41131156","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 1

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 结直肠癌、SARS-CoV-2 和肺损伤小鼠模型中 [11C]evobrutinib 的初步 PET 成像：通过碱辅助钯-NiXantphos 介导的 11C 羧化进行放射合成。

IF 0.9 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2023-09-10 DOI: 10.1002/jlcr.4062

Amanda J. Boyle, Anton Lindberg, Junchao Tong, Dongxu Zhai, Fang Liu, Neil Vasdev

{"title":"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","authors":"Amanda J. Boyle, Anton Lindberg, Junchao Tong, Dongxu Zhai, Fang Liu, Neil Vasdev","doi":"10.1002/jlcr.4062","DOIUrl":"10.1002/jlcr.4062","url":null,"abstract":"Evobrutinib is a second-generation, highly selective, irreversible Bruton's tyrosine kinase (BTK) inhibitor that has shown efficacy in the autoimmune diseases arthritis and multiple sclerosis. Its development as a positron emission tomography (PET) radiotracer has potential for in vivo imaging of BTK in various disease models including several cancers, severe acute respiratory syndrome-coronavirus-2 (SARS-CoV-2), and lipopolysaccharide (LPS)-induced lung damage. Herein, we report the automated radiosynthesis of [11C]evobrutinib using a base-aided palladium-NiXantphos-mediated 11C-carbonylation reaction. [11C]Evobrutinib was reliably formulated in radiochemical yields of 5.5 ± 1.5% and a molar activity of 34.5 ± 17.3 GBq/μmol (n = 12) with 99% radiochemical purity. Ex vivo autoradiography studies showed high specific binding of [11C]evobrutinib in HT-29 colorectal cancer mouse xenograft tissues (51.1 ± 7.1%). However, in vivo PET/computed tomography (CT) imaging with [11C]evobrutinib showed minimal visualization of HT-29 colorectal cancer xenografts and only a slight increase in radioactivity accumulation in the associated time-activity curves. In preliminary PET/CT studies, [11C]evobrutinib failed to visualize either SARS-CoV-2 pseudovirus infection or LPS-induced injury in mouse models. In conclusion, [11C]evobrutinib was successfully synthesized by 11C-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.","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"67 6","pages":"235-244"},"PeriodicalIF":0.9,"publicationDate":"2023-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/jlcr.4062","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10168412","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

[68Ga]Ga-PentixaFor: Development of a fully automated in hospital production on the Trasis miniAllinOne synthesizer [68Ga]Ga PentixaFor：在Trasis miniAlliOne合成器上开发全自动医院生产

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2023-09-07 DOI: 10.1002/jlcr.4061

Julien Costes, Kilian Casasagrande, Constance Dubegny, Juan Castillo, Jens Kaufman, Julien Masset, Charles Vriamont, Corentin Warnier, Alain Faivre-Chauvet, Judith Anna Delage

{"title":"[68Ga]Ga-PentixaFor: Development of a fully automated in hospital production on the Trasis miniAllinOne synthesizer","authors":"Julien Costes, Kilian Casasagrande, Constance Dubegny, Juan Castillo, Jens Kaufman, Julien Masset, Charles Vriamont, Corentin Warnier, Alain Faivre-Chauvet, Judith Anna Delage","doi":"10.1002/jlcr.4061","DOIUrl":"https://doi.org/10.1002/jlcr.4061","url":null,"abstract":"[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 needs, an automatized synthesis process ensuring efficient and reproducible production and improving operator's radioprotection is needed. [68Ga]Ga-PentixaFor synthesis has been described on other synthesizers but not on the miniAiO. In this work, we defined automated synthesis process and an analytical method for the quality control of [68Ga]Ga-PentixaFor. Validation batches were performed under aseptic conditions in a class A hotcell. All the quality controls required by the European Pharmacopea (Eur. Ph) were performed. The analytical methods were validated according to the International Conference Harmonization (ICH) recommendations. Validation batches were performed with a radiochemical yield of 94.8 ± 2.6%. All the quality controls were in conformity with the Eur. Ph, and the validation of the analytical method complied with the ICH. The environmental monitoring performed during the synthesis process showed that the aseptic conditions were ensured. [68Ga]Ga-PentixaFor was successfully synthesized with the miniAiO by a fully automated process. This robust production mode and the quality control have been validated in this study allowing to increase the access of patients to this new promising radiopharmaceutical.","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"66 12","pages":"400-410"},"PeriodicalIF":1.8,"publicationDate":"2023-09-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/jlcr.4061","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"50124585","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0