Journal of labelled compounds & radiopharmaceuticals最新文献

Correction to “A Practical Radiosynthesis of (S)-[11C]SMBT-1 for MAO-B PET Imaging” 更正“(S)-[11C]SMBT-1用于MAO-B PET成像的实用放射性合成”。

IF 1.3 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-10-16 DOI: 10.1002/jlcr.70043

引用次数: 0

Synthesis of USP Grade [2,3,7-13C3]-Nicotinamide for Human Pharmacokinetic Studies USP级[2,3,7- 13c3]-烟酰胺的合成及人药代动力学研究

IF 1.3 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-10-09 DOI: 10.1002/jlcr.70041

Bruce G. Szczepankiewicz, Karsten J. Koppetsch, Michael P. Drolet, David Cao, Jonathan N. Kremsky, Eric E. Buck, George Rotsides, Greg Griffin, Siead Zegar, Alan Henderson, David J. Livingston

引用次数: 0

Synthesis of a C-14 Labeled Heme C-14标记血红素的合成

IF 1.3 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-10-07 DOI: 10.1002/jlcr.70042

Cecilia Ericsson, Jonas Bergare, Charles S. Elmore

引用次数: 0

Simple and Efficient Automated Radiosynthesis of 1-[18F]-IPA Using Solid-Phase Extraction Cartridges Purification 用固相萃取筒提纯1-[18F]- ipa的简单高效自动放射性合成

IF 1.3 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-09-21 DOI: 10.1002/jlcr.70040

Weixuan Dong, Cong Shen, Ruxi Chang, Zhewei Zhang, Chen Niu, Xiaoyi Duan

{"title":"Simple and Efficient Automated Radiosynthesis of 1-[18F]-IPA Using Solid-Phase Extraction Cartridges Purification","authors":"Weixuan Dong, Cong Shen, Ruxi Chang, Zhewei Zhang, Chen Niu, Xiaoyi Duan","doi":"10.1002/jlcr.70040","DOIUrl":"10.1002/jlcr.70040","url":null,"abstract":"<div>\u0000 \u0000 1-[18F]Fluoroethyl-indole propionic acid (1-[18F]-IPA), a fluorinated analogue of indole-3-propionic acid (IPA), shows considerable promise as a PET tracer for imaging BxPC-3 pancreatic cancer xenografts. In the present study, we report a straightforward automated synthesis protocol that employs cartridge-based purification, providing 1-[18F]-IPA in a form suitable for human use. This method was developed in compliance with good manufacturing practice (GMP) guidelines, and the final product meets the established release specifications for radiopharmaceuticals. The automated synthesis was carried out via a two-step, one-pot procedure, which involved [18F]fluorination of methyl 1-(2-tosyloxyethyl)-1H-indole-3-propionate, subsequent hydrolysis with sodium hydroxide, and purification using a series of commercially available solid-phase extraction cartridges, thereby eliminating the need for preparative high-performance liquid chromatography (preparative HPLC). Using this one-pot approach on a modified commercial GE TRACERlab FX-FN radiosynthesis module, the final product was obtained with high uncorrected radiochemical yields (> 35 %) and radiochemical purity (> 95 %). Collectively, these results establish the GE TRACERlab FX-FN radiosynthesis module as a robust, flexible, and cost-effective platform for the routine clinical production of 1-[18F]-IPA.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 10-11","pages":""},"PeriodicalIF":1.3,"publicationDate":"2026-09-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149017091","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

A Practical Radiosynthesis of (S)-[11C]SMBT-1 for MAO-B PET Imaging (S)-[11C]SMBT-1在MAO-B PET成像中的应用

IF 1.3 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-09-08 DOI: 10.1002/jlcr.70037

Hari K. Akula, Soumyaranjan Pati, Wenchao Qu, Mark Slifstein, Ramin Parsey, Ryuichi Harada, Shozo Furumoto, Nobuyuki Okamura, Min-Jeong Kim, Bao Hu

{"title":"A Practical Radiosynthesis of (S)-[11C]SMBT-1 for MAO-B PET Imaging","authors":"Hari K. Akula, Soumyaranjan Pati, Wenchao Qu, Mark Slifstein, Ramin Parsey, Ryuichi Harada, Shozo Furumoto, Nobuyuki Okamura, Min-Jeong Kim, Bao Hu","doi":"10.1002/jlcr.70037","DOIUrl":"10.1002/jlcr.70037","url":null,"abstract":"<div>\u0000 \u0000 Monoamine oxidase B (MAO-B) is highly expressed in reactive astrocytes and is implicated in multiple neurodegenerative and neuropsychiatric conditions, making it an important PET imaging target. Building on the promising PET imaging properties of (S)-(2-methylpyrid-5-yl)-6-[(3-18F-fluoro-2-hydroxy)propoxy]quinoline ((S)-[18F]SMBT-1), we developed a carbon-11-labeled analog, (S)-(2-11C-methylpyrid-5-yl)-6-[(3-fluoro-2-hydroxy)propoxy]quinoline ((S)-[11C]SMBT-1). The short half-life of carbon-11 (t1/2 = 20.7 min) enables same-day, repeat scans and pharmacological challenge studies within the same subject. An efficient radiosynthesis of (S)-[11C]SMBT-1 was developed via palladium-mediated Stille cross-coupling followed by acid deprotection. The radiosynthesis was completed within 28.4 ± 0.9 min from end of bombardment (EOB) (n = 3), providing (S)-[11C]SMBT-1 in 11.9% ± 2.7% radiochemical yield (decay-corrected) with final product activity of 1.76 ± 0.28 GBq (47.4 ± 7.5 mCi) and molar activity of 58.8 ± 8.0 GBq/μmol (1.59 ± 0.22 Ci/μmol) at end of synthesis (EOS), high radiochemical purity (> 99%) and enantiomeric excess (> 99%). The developed radiosynthetic method provides reliable access to (S)-[11C]SMBT-1, and in vivo evaluation studies are currently underway to further assess its potential for future clinical MAO-B PET imaging applications.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 10-11","pages":""},"PeriodicalIF":1.3,"publicationDate":"2026-09-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148912218","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

Multistep Continuous Flow Synthesis of 14C-Labeled cis/trans-Chrysanthemic Acid 14c标记的顺式/反式菊花酸的多步连续合成

IF 1.3 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-09-07 DOI: 10.1002/jlcr.70038

Shota Hashino, Takaaki Kobayashi, Motohiro Kurosawa, Takuo Fujisawa

{"title":"Multistep Continuous Flow Synthesis of 14C-Labeled cis/trans-Chrysanthemic Acid","authors":"Shota Hashino, Takaaki Kobayashi, Motohiro Kurosawa, Takuo Fujisawa","doi":"10.1002/jlcr.70038","DOIUrl":"10.1002/jlcr.70038","url":null,"abstract":"<div>\u0000 \u0000 Natural pyrethrins and their analogues, synthetic pyrethroids, are widely used insecticides due to rapid action and broad efficacy. For tracer studies to comprehensively assess their safety, carbon-14 (14C)–labeled compounds are required. However, the conventional batch synthesis of 14C-labeled chrysanthemic acid—a key precursor for labeled pyrethroids—poses several challenges, including the handling of explosive and volatile intermediates, the management of safety concerns, and radioactive contamination risk. To address these issues, we have developed the first multistep continuous flow synthesis of 14C-labeled cis/trans-chrysanthemic acid. Our approach utilizes a series of sealed devices to perform diazotization, rhodium (Rh)–catalyzed cyclopropanation, hydrolysis, and continuous extractive workup without isolating hazardous intermediates. This setup enables safe, efficient, and scalable production, as the continuous flow system allows direct transfer between reaction steps and the rapid adjustment of scale by modulating feed rates. The newly developed flow synthesis of 14C-labeled cis/trans-chrysanthemic acid demonstrated significantly reduced safety concerns and the risk of radioactive contamination and improved operational efficiency compared with the conventional batch method.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 10-11","pages":""},"PeriodicalIF":1.3,"publicationDate":"2026-09-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148906406","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

Synthesis and Characterization of 2-(1-Hydroxyethyl)Promazine Sulfoxide-d4 HCl as an Internal Standard for the Accurate Quantitation of 2-(1-Hydroxyethyl)Promazine Sulfoxide in Equine Urine 2-（1-羟乙基）丙嗪亚砜-d4 HCl的合成及表征作为马尿中2-（1-羟乙基）丙嗪亚砜准确定量的内标

IF 1.3 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-09-01 DOI: 10.1002/jlcr.70036

Justin C. Holmes, Ballard C. Smith, Samuel G. Awuah, Rodney Eisenberg, Andreas F. Lehner, Clara K. Fenger, George A. Maylin, Kimberly Brewer, Thomas Tobin

{"title":"Synthesis and Characterization of 2-(1-Hydroxyethyl)Promazine Sulfoxide-d4 HCl as an Internal Standard for the Accurate Quantitation of 2-(1-Hydroxyethyl)Promazine Sulfoxide in Equine Urine","authors":"Justin C. Holmes, Ballard C. Smith, Samuel G. Awuah, Rodney Eisenberg, Andreas F. Lehner, Clara K. Fenger, George A. Maylin, Kimberly Brewer, Thomas Tobin","doi":"10.1002/jlcr.70036","DOIUrl":"10.1002/jlcr.70036","url":null,"abstract":"<div>\u0000 \u0000 Acetylpromazine, 1-{10-[3-(dimethylamino)propyl]-10H-phenothiazin-2-yl}ethenone, C19H22N2OS, 326.46 g·mol−1 is a phenothiazine derivative at one time used in human medicine as an antipsychotic medication but now predominantly used in veterinary medicine as a sedative/tranquilizer and referred to as acepromazine. In performance horses its use is regulated by using a 10 ng/mL threshold for the major urinary metabolite 2-(1-hydroxyethyl) promazine-sulfoxide (HEPS) in equine urine. To enable accurate quantitation of HEPS in equine urine we have synthesized and purified hydroxyethylpromazine sulfoxide-d4 (HEPS-d4) to be used as a stable isotopically labeled internal standard. Although labeled HEPS is commercially available (CAS 1346605-30-8), to the best of our knowledge there is no published synthetic procedure in the scientific literature. Here we demonstrate a viable synthetic procedure consisting of four major steps: (i) freebasing the Acepromazine maleate salt, (ii) H-D exchange of Acepromazine at room temperature, (iii) reduction of the ketone with NaBD4, and (iv) oxidation of the thioether via hydrogen peroxide and acetic acid. This deuterated internal standard will allow for precise LC/MS quantitation of HEPS at regulatory threshold concentrations, enabling accurate detection and quantitation of picogram/mL concentrations in equine urine samples, thereby supporting regulatory compliance for equine medication control programs.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 10-11","pages":""},"PeriodicalIF":1.3,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148865371","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

Reliable One-Pot Automated Preparation of [11C]SL25.1188 for Use in Clinical Imaging Studies 可靠的一锅自动制备[11C]SL25.1188用于临床影像学研究

IF 1.3 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-08-21 DOI: 10.1002/jlcr.70035

Hiroki Hashimoto, Takayuki Ohkubo, Kaito Tsukagoe, Tomoya Fujishiro, Daisuke Arashi, Tatsuto Sato, Takeru Seki, Yusuke Kurihara, Masanao Ogawa, Masatoshi Muto, Nobuki Nengaki, Wakana Mori, Masayuki Fujinaga, Kazunori Kawamura, Ming-Rong Zhang

{"title":"Reliable One-Pot Automated Preparation of [11C]SL25.1188 for Use in Clinical Imaging Studies","authors":"Hiroki Hashimoto, Takayuki Ohkubo, Kaito Tsukagoe, Tomoya Fujishiro, Daisuke Arashi, Tatsuto Sato, Takeru Seki, Yusuke Kurihara, Masanao Ogawa, Masatoshi Muto, Nobuki Nengaki, Wakana Mori, Masayuki Fujinaga, Kazunori Kawamura, Ming-Rong Zhang","doi":"10.1002/jlcr.70035","DOIUrl":"https://doi.org/10.1002/jlcr.70035","url":null,"abstract":"<div>\u0000 \u0000 We clinically investigated (S)-5-methoxymethyl-3-[6-(4,4,4-trifluorobutoxy)benzo[d]isoxazol-3-yl]oxazolidin-2-[11C]-one ([11C]SL25.1188) as a positron emission tomography tracer for imaging monoamine oxidase B. To perform clinical imaging studies at our institute, we established a routine method for preparing the [11C]SL25.1188 injection using a one-pot [11C]CO2 fixation method. We successfully prepared the [11C]SL25.1188 injection using a 11C-labeling synthesizer and sterile isolator. The radiosynthesis time and decay-corrected radiochemical yield based on [11C]CO2 were below 30 min and 49% ± 10% postirradiation (n = 104), respectively. At the end of synthesis (n = 104), the molar activity was 180 ± 57 GBq/μmol, and the radiochemical purity exceeded 99%. The results of [11C]SL25.1188 injection complied fully with our in-house quality control and quality assurance criteria, confirming a reliable supply of high-quality [11C]SL25.1188 formulation with adequate radioactivity for use in clinical imaging studies.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 10-11","pages":""},"PeriodicalIF":1.3,"publicationDate":"2026-08-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148784742","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

Gram-Scale Synthesis of Perdeuterated Paracetamol 克级合成过氘化扑热息痛

IF 1.3 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-08-04 DOI: 10.1002/jlcr.70034

Alexander Park, Robert M. Edkins, June McCorquodale, James Tellam, Sarah Youngs, Katharina Edkins

{"title":"Gram-Scale Synthesis of Perdeuterated Paracetamol","authors":"Alexander Park, Robert M. Edkins, June McCorquodale, James Tellam, Sarah Youngs, Katharina Edkins","doi":"10.1002/jlcr.70034","DOIUrl":"https://doi.org/10.1002/jlcr.70034","url":null,"abstract":"The synthesis of deuterated compounds is a major stumbling block in the field of neutron total scattering on disordered materials. This is due to the requirement for large quantities of pure sample with high deuterium content across all positions. Typical deuterations in literature focus on site-specific deuterations typically on milligram scales. Here, we successfully synthesised paracetamol-d9, as well as its related isotopologues, on a multigram scale. We proceeded through an acid-catalysed deuteration of 4-aminophenol under microwave irradiation. We were able to efficiently purify the unstable intermediate, 4-aminophenol-d4 by sublimation, which meant we could avoid the formation of strongly coloured impurities that could not be removed from the final product otherwise. The pure intermediate then underwent acetylation with a 75% yield. More than 10 g of the final perdeuterated product was synthesised with an average deuterium incorporation of > 93% and no less than 78% at any individual position.","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 10-11","pages":""},"PeriodicalIF":1.3,"publicationDate":"2026-08-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/jlcr.70034","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148662478","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

Synthesis of Potent Vanin-1 Inhibitors Labelled With Carbon-14 and Deuterium 碳-14和氘标记强效Vanin-1抑制剂的合成。

IF 1.3 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2026-07-09 DOI: 10.1002/jlcr.70033

Bachir Latli, Matt Hrapchak, Ling Wu, Lalith Samankumara, Jaehee Lee, Bo Qu

{"title":"Synthesis of Potent Vanin-1 Inhibitors Labelled With Carbon-14 and Deuterium","authors":"Bachir Latli, Matt Hrapchak, Ling Wu, Lalith Samankumara, Jaehee Lee, Bo Qu","doi":"10.1002/jlcr.70033","DOIUrl":"10.1002/jlcr.70033","url":null,"abstract":"<div>\u0000 \u0000 Vanin-1 is an enzyme highly expressed in the kidneys, liver, and small intestines. Inhibition of this enzyme has been postulated as a novel approach in the treatment of several inflammatory diseases. BI 764122, BI 1585773, and BI 1595043 are very potent inhibitors of this enzyme. These three analogs share the same (S)-N-(nicotinoyl)pyrrolidin-3-yl)-N-methyl acetamide moiety. The preparation of these analogs labelled with carbon-14 was accomplished via carbon-14 carboxylation with carbon dioxide of corresponding aryl halides, followed by amide bond formation with (S)-N-(methyl)-N-(pyrrolidin-3-yl)acetamide. For metabolic considerations, the radioactive carbon was also incorporated in a cyclopropyl in [14C]-BI 764122 synthesis. The deuterium labelling of these three compounds was completed using the common moiety (S)-N-(methyl-d3)-N-(pyrrolidin-3-yl)acetamide-d3, which was prepared in three steps and then coupled to the corresponding aryl acids via amide bond.\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 9","pages":""},"PeriodicalIF":1.3,"publicationDate":"2026-07-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148411973","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