Journal of labelled compounds & radiopharmaceuticals最新文献_第10页

Benzylic deuteration of alkylnitroaromatics via amine-base catalysed exchange with deuterium oxide 胺基氧化氘催化交换烷基硝基芳烃的苯代氘化

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2022-12-01 DOI: 10.1002/jlcr.4008

Stephen Maddocks, Nurul F. Samuri, Katerina Ridge, Ian D. Cunningham, William J. S. Lockley

{"title":"Benzylic deuteration of alkylnitroaromatics via amine-base catalysed exchange with deuterium oxide","authors":"Stephen Maddocks, Nurul F. Samuri, Katerina Ridge, Ian D. Cunningham, William J. S. Lockley","doi":"10.1002/jlcr.4008","DOIUrl":"10.1002/jlcr.4008","url":null,"abstract":"This paper describes the deuterium-labelling of alkylnitroaromatics by base-catalysed exchange with deuterium oxide. As the alkyl protons alpha to the aromatic ring are the most acidic sites in the molecule, regioselective hydrogen isotope exchange at this benzylic location leads to a regiospecifically deuterated product. The exchange labelling takes place in good yields and with high atom% abundance in the presence of an appropriate nitrogen base. Alkylated 2,4-dinitrobenzenes deuterate at room temperature under catalysis by triethylamine, whilst alkylated 2-nitro- or 4-nitrobenzenes and related mono-nitroaromatics require higher temperatures and catalysis by 1,5-diazobicyclo[4.3.0]non-5-ene (DBN). The labelling reactions require an inert gas atmosphere, but otherwise are simple and high yielding with no obvious byproducts. Those compounds in which the benzylic protons are in an ortho-orientation with respect to the nitro group label somewhat more slowly than the analogues where there is a para relationship. In addition, higher alkyl homologues undergo benzylic deuteration at slower rates than methyl.","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"66 1","pages":"11-21"},"PeriodicalIF":1.8,"publicationDate":"2022-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://analyticalsciencejournals.onlinelibrary.wiley.com/doi/epdf/10.1002/jlcr.4008","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9375791","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

Carbon-13 labeling of ibrutinib for human microdosing 依鲁替尼用于人体微剂量的碳-13标记

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2022-11-22 DOI: 10.1002/jlcr.4007

Yong Gong, Rhys Salter

引用次数: 0

The synthesis of deuteriated tri-tert-butyl phosphine. 氘化三叔丁基膦的合成。

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2022-11-01 DOI: 10.1002/jlcr.4001

Lucy C Brown, Anne McGrogan, Yoan Delavoux, James M Hogg, John D Holbrey, H Q Nimal Gunaratne, Małgorzata Swadźba-Kwaśny, James P Tellam, Sarah E Youngs

引用次数: 0

A flow electrochemistry-enabled synthesis of 2-substituted N-(methyl-d)piperidines 流动电化学合成2-取代N-(甲基-d)哌啶

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2022-10-22 DOI: 10.1002/jlcr.4006

Azzam A. M. AL-Hadedi, Stuart Sawyer, Stuart J. Elliott, Robert A. Green, Daniel J. O'Leary, Richard C. D. Brown, Lynda J. Brown

引用次数: 0

In vivo and in vitro binding of [125I]I-R-(+)-TISCH: A dopamine D1 receptor ligand for studying pancreatic β-cell mass [125I]I-R-(+)- tisch:一种多巴胺D1受体配体在体内和体外结合研究胰腺β细胞质量

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2022-10-19 DOI: 10.1002/jlcr.4005

Yan Zhang, Guangwen Li, Yuli Sun, Haiyan Hong, Linlin Li, Yang Luo, Ran Wang, Lin Zhu, Hank F. Kung, Jinxia Zhu

{"title":"In vivo and in vitro binding of [125I]I-R-(+)-TISCH: A dopamine D1 receptor ligand for studying pancreatic β-cell mass","authors":"Yan Zhang, Guangwen Li, Yuli Sun, Haiyan Hong, Linlin Li, Yang Luo, Ran Wang, Lin Zhu, Hank F. Kung, Jinxia Zhu","doi":"10.1002/jlcr.4005","DOIUrl":"10.1002/jlcr.4005","url":null,"abstract":"Diabetes mellitus (DM) and insulinoma are mainly affected by the status of pancreatic β-cell mass (BCM). Development of imaging agents for BCM allows to study pancreatic β cells and the relationship between β cells and DM or insulinoma. In this study, we investigated the density of dopamine D1 receptor on the β cells and measured BCM by statistical image processing. The pancreatic uptakes of [125I]I-R-(+)-7-chloro-8-hydroxy-1-(3′-iodopheny1)-3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine ([125I]I-R-(+)-TISCH), dopamine D1 receptor tracer, in normal and diabetic rats displayed significant differences at 30 min (1.11 ± 0.08% ID/g vs. 0.63 ± 0.09% ID/g, p < 0.0001). In the presence of SCH23390, the pancreatic uptake of [125I]I-R-(+)-TISCH at 30 min in normal rats was lower (1.01 ± 0.04% ID/g, p < 0.05). Although the blocking was not complete, [125I]I-R-(+)-TISCH showed specific binding signals to the pancreas. Furthermore, the uptakes of [125I]I-R-(+)-TISCH in INS-1 cells were reduced in the presence of SCH23390 at different concentrations. [125I]I-R-(+)-TISCH displayed a respectable uptake in insulinoma. Overall, [125I]I-R-(+)-TISCH provided specific binding signals to pancreatic β cells. Although the specific signal may not be sufficient for imaging in vivo, the dopamine D1 receptor can still be considered as a potential target for studying BCM. Further investigation will be required to optimize the ligand.","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"65 14","pages":"354-360"},"PeriodicalIF":1.8,"publicationDate":"2022-10-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10442209","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

Good manufacturing procedure production of [18F]SynVesT-1, a radioligand for in vivo positron emission tomography imaging of synaptic vesicle glycoprotein 2A 良好的生产程序生产[18F]SynVesT-1，一种用于突触囊泡糖蛋白2A体内正电子发射断层成像的放射配体

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2022-08-31 DOI: 10.1002/jlcr.4002

Kenneth Dahl, Stefan Larsson, Peter Bonn, Anita Wallin, Oleksiy Itsenko, Michael Schöll

{"title":"Good manufacturing procedure production of [18F]SynVesT-1, a radioligand for in vivo positron emission tomography imaging of synaptic vesicle glycoprotein 2A","authors":"Kenneth Dahl, Stefan Larsson, Peter Bonn, Anita Wallin, Oleksiy Itsenko, Michael Schöll","doi":"10.1002/jlcr.4002","DOIUrl":"10.1002/jlcr.4002","url":null,"abstract":"[18F]SynVesT-1 (also known as [18F]SDM-8 or [18F]MNI-1126) is a potent and selective synaptic vesicle glycoprotein 2 (SV2A) positron emission tomography (PET) imaging agent. In order to fulfill the increasing clinical demand of an 18F-labeled SV2A PET ligand, we have developed a fully automated procedure to provide a sterile and pyrogen-free good manufacturing procedure (GMP)-compliant product of [18F]SynVesT-1 suitable for clinical studies in humans. [18F]SynVesT-1 is synthesized via a rapid copper-mediated radiofluorination protocol. The procedure was developed and established on a commercially available module, TracerMaker (ScanSys Laboratorieteknik ApS, Copenhagen, Denmark), a synthesis platform originally developed to conduct carbon-11 radiochemistry. From ~130 GBq (end-of-bombardment), our newly developed procedure enabled us to prepare [18F]SynVesT-1 in an isolated radioactivity yield of 14,220 ± 800 MBq (n = 3), which corresponds to a radiochemical yield (RCY) of 19.5 ± 0.5%. The radiochemical purity (RCP) and enantiomeric purity of each of the final formulated batches exceeded 98%. The overall synthesis time was 90 min and the molar activity was 330 ± 60 GBq/μmol (8.9 ± 1.6 Ci/μmol). The produced [18F]SynVesT-1 was stable over 8 h at room temperature and is suitable for in vivo PET imaging studies in human subjects.","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"65 12","pages":"315-322"},"PeriodicalIF":1.8,"publicationDate":"2022-08-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40334401","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

An improved radiosynthesis of [18F]FAraG, a PET radiotracer for imaging T-cell activation 一种用于成像t细胞激活的PET放射性示踪剂[18F]FAraG的改进放射合成

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2022-08-24 DOI: 10.1002/jlcr.3999

Daniel P. Holt, Robert F. Dannals

引用次数: 0

Low-scale syringe-made synthesis of 15N-labeled oligonucleotides 小型注射器合成15n标记的寡核苷酸

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2022-08-24 DOI: 10.1002/jlcr.4000

Břetislav Brož, František Tureček, Aleš Marek

引用次数: 1

Highly effective liquid and solid phase extraction methods to concentrate radioiodine isotopes for radioiodination chemistry. 高效液相和固相萃取法浓缩放射性碘同位素，用于放射性碘化学。

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2022-08-01 DOI: 10.1002/jlcr.3994

Christopher Davis, Chun Li, Ruirui Nie, Norman Guzzardi, Barbara Dworakowska, Pragalath Sadasivam, John Maher, Eric O Aboagye, Zhi Lu, Ran Yan

引用次数: 1

Simplified and accessible [¹⁸ F]F-AraG synthesis procedure for preclinical PET. 临床前PET的F- arag合成过程的简化和易于获取[18 F]。

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2022-08-01 DOI: 10.1002/jlcr.3997

Antonia A Högnäsbacka, Miguel A Cortés González, Christer Halldin, Magnus Schou

引用次数: 1