Efficient syntheses of [¹¹C]zidovudine and its analogs by convenient one-pot palladium(0)-copper(I) co-mediated rapid C-[¹¹C]methylation.

abstract：:As part of a program toward making analogues of amlexanox (1), currently under clinical investigation for the treatment of type 2 diabetes and obesity, we have synthesized derivative 5 in which deuterium has been introduced into two sites of metabolism on the C-7 isopropyl function of amlexanox. The synthesis of 5 was...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Gan X,Wilson MW,Beyett TS,Wen B,Sun D,Larsen SD,Tesmer JJG,Saltiel AR,Showalter HD

更新日期：2019-05-15 00:00:00

abstract：:A robust medium-scale (approximately 3 g) synthetic method for 15 N labeling of pyridine (15 N-Py) is reported based on the Zincke reaction. 15 N enrichment in excess of 81% was achieved with approximately 33% yield. 15 N-Py serves as a standard substrate in a wide range of studies employing a hyperpolarization techni...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Chukanov NV,Kidd BE,Kovtunova LM,Bukhtiyarov VI,Shchepin RV,Chekmenev EY,Goodson BM,Kovtunov KV,Koptyug IV

更新日期：2019-11-01 00:00:00

abstract：:Palladium(II)-mediated oxidative carbonylation reactions have been used to synthesize (11) C-radiolabelled ureas via the coupling of amines with [(11) C]carbon monoxide, in a one-pot process. Following trapping of (11) CO in a solution of copper(I) tris(3,5-dimethylpyrazolyl)borate, homocoupling reactions of primary a...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Kealey S,Husbands SM,Bennacef I,Gee AD,Passchier J

更新日期：2014-04-01 00:00:00

abstract：:With the recent ability to use combined liquid chromatography/electrospray tandem mass spectrometry to analyze for several eicosanoids in biological samples in a single and rapid experiment, heavy isotope-labeled eicosanoids are needed as internal standards in order to quantify eicosanoid analytes. The present study d...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Ghomashchi F,Bollinger JG,Gelb MH

更新日期：2007-07-17 00:00:00

abstract：:Enzalutamide, a second-generation antiandrogen, has been developed for the treatment of castration-resistance prostate cancer. We synthesized the deuterated analogues 6 and found that it showed higher drug exposure and thus stronger antitumor potency in preclinical settings. Compound 6 is being developed clinically fo...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Pang X,Peng L,Chen Y

更新日期：2017-07-01 00:00:00

abstract：:Therapy for human immunodeficiency virus (HIV)-infected patients requires chronic multidrug administration. The eventual failure of therapy in some patients has brought into question the tissue concentration of the drugs. With an appropriately radiolabeled compound, we could utilize positron emission tomography to pro...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Kiesewetter DO,Knudson K,Collins M,Srinivasula S,Lim E,Di Mascio M

更新日期：2008-03-13 00:00:00

abstract：:Pyropheophorbide-a (Pyro) is a promising multifunctional molecule for multimodal tumour imaging and photodynamic therapy, but its clinical applications are seriously restricted by the limited tumour accumulation capability. Here, we designed and synthesized a small-molecule probe that achieved specific dual-modal tumo...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Fan D,Wang K,Gao H,Luo Q,Wang X,Li X,Tong W,Zhang X,Luo C,Yang G,Ai L,Shi J

更新日期：2020-05-15 00:00:00

abstract：:Insulinomas, neuroendocrine tumors arising from pancreatic beta cells, often show overexpression of the glucagon-like peptide-1 receptor. Therefore, imaging with glucagon-like peptide analog exendin-4 can be used for diagnosis and preoperative localization. This review presents an overview of the development and clini...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Jansen TJP,van Lith SAM,Boss M,Brom M,Joosten L,Béhé M,Buitinga M,Gotthardt M

更新日期：2019-08-01 00:00:00

abstract：:This open-label, single-period study in healthy subjects estimated evacetrapib absolute bioavailability following simultaneous administration of a 130-mg evacetrapib oral dose and 4-h intravenous (IV) infusion of 175 µg [(13) C8 ]-evacetrapib as a tracer. Plasma samples collected through 168 h were analyzed for evacet...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Cannady EA,Aburub A,Ward C,Hinds C,Czeskis B,Ruterbories K,Suico JG,Royalty J,Ortega D,Pack BW,Begum SL,Annes WF,Lin Q,Small DS

更新日期：2016-05-30 00:00:00

abstract：:Flavin nucleotides, i.e. flavin mononucleotide (FMN) and flavin adenine dinucleotide (FAD), are utilized as prosthetic groups and/or substrates by a myriad of proteins, ranging from metabolic enzymes to light receptors. Isotopically labeled flavins have served as invaluable tools in probing the structure and function ...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Mishanina TV,Kohen A

更新日期：2015-07-01 00:00:00

abstract：:Labeling agents with radioisotopes or fluorescent dyes are useful for investigating the biodistributions of biologically active proteins and peptides. Compared with molecular imaging with a single modality, dual imaging probes provide complementary information for each modality. The development of a dual radioisotope/...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Watanabe H,Itagaki F,Shimizu Y,Iikuni S,Ono M

更新日期：2019-11-01 00:00:00

abstract：:[15 N]-Cholamine is an isotope tag for metabolomics research, because it possesses 2 important properties: an NMR active isotope and a permanent charge for MS sensitivity. Here, we present a scalable synthesis of [15 N]-cholamine. ...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Szeto J,Lemoine R,Nguyen R,Olson LL,Tanga MJ

更新日期：2018-04-01 00:00:00

abstract：:Internal therapy with α-emitters should be well suited for micrometastatic disease. Radium-224 emits multiple α-particles through its decay and has a convenient 3.6 days of half-life. Despite its attractive properties, the use of 224 Ra has been limited to bone-seeking applications because it cannot be stably bound to...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Westrøm S,Malenge M,Jorstad IS,Napoli E,Bruland ØS,Bønsdorff TB,Larsen RH

更新日期：2018-05-30 00:00:00

abstract：:In this study, we developed a saccharin (SAC)-based radiopharmaceutical (68 Ga-NOTA-SAC) and evaluated the possibility of its application as a PET tracer in the diagnosis of carbonic anhydrase IX (CA IX)-overexpressed tumors. We did a water-soluble tetrazolium assay and flow cytometry analysis to identify the cell via...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Shin UC,Choi JS,Beak YJ,Lee MW,Kim HS,Choi DW,Kim DG,Kim SW

更新日期：2020-10-29 00:00:00

abstract：:A decline of norepinephrine transporter (NET) level is associated with several psychiatric and neurological disorders. Therefore positron emission tomography (PET) imaging agents are greatly desired to study the NET pathway. We have developed a C-fluoropropyl analog of nisoxetine: (R)-N-methyl-3-(3'-[(18)F]fluoropropy...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Nguyen VL,Pichika R,Bhakta PH,Kant R,Mukherjee J

更新日期：2010-02-09 00:00:00

abstract：:Metabolism, environmental fate, and low concentration food residue studies would be facilitated by the use of radiolabeled test articles that can be readily quantified within complex matrices. However, radiochemical approaches for such studies require high specific activities to allow analytical detection of correspon...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Singh A,Hakk H,Lupton SJ

更新日期：2018-04-01 00:00:00

abstract：:Bruton's tyrosine kinase (BTK) is a key component in the B-cell receptor signaling pathway and is consequently a target for in vivo imaging of B-cell malignancies as well as in multiple sclerosis (MS) with positron emission tomography (PET). A recent Phase 2b study with Sanofi's BTK inhibitor, Tolebrutinib (also known...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Dahl K,Turner T,Vasdev N

更新日期：2020-09-01 00:00:00

abstract：:Herein, we report a short, three-step synthesis of d-[1-(14) C]-serine (4) in high enantiomeric purity. Starting from [(14) C]-KCN and 2-(benzyloxy)acetaldehyde, Strecker reaction using (R)-1-phenylethylamine as the chiral auxiliary gave two diastereomeric aminonitriles 1 and 2 in the ratio of 4:3, which were convenie...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Song F,Salter R,Weaner LE

更新日期：2015-04-01 00:00:00

abstract：:Changes in the magnitude of the mitochondrial membrane potential occur in a range of important pathologies. To assess changes in membrane potential in patients, we set out to develop an improved mitochondria-targeted positron emission tomography probe comprising a lipophilic triphenylphosphonium cation attached to a f...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Li L,Brichard L,Larsen L,Menon DK,Smith RA,Murphy MP,Aigbirhio FI

更新日期：2013-12-01 00:00:00

abstract：:An agonist PET tracer is of key interest for the imaging of the 5-HT2A receptor, as exemplified by the previously reported success of [11 C]Cimbi-36. Fluorine-18 holds several advantages over carbon-11, making it the radionuclide of choice for clinical purposes. In this respect, an 18 F-labelled agonist 5-HT2A recepto...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Edgar FG,Hansen HD,Leth-Petersen S,Ettrup A,Kristensen JL,Knudsen GM,Herth MM

更新日期：2017-10-01 00:00:00

abstract：:Ulcerative colitis is a chronic disease having a regressive nature. Commonly used diagnostic methods have the disadvantage to be invasive, time-consuming, and expensive. Therefore, a new sensitive method for the detection and monitoring of disease activity is urgently needed in clinical practice. In the current invest...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： El-Kawy OA,Ibrahim IT,Farah K

更新日期：2015-06-30 00:00:00

abstract：:3-Amino-4-(1,1-difluoro-propyl)-6-(4-methanesulfonyl-piperidin-1-yl)-thieno[2,3-b]pyridine-2-carboxylic acid amide (1) is a potent IκB Kinase-β (IKK-β) inhibitor. The efficient preparations of this compound labeled with carbon-14 and deuterium are described. The carbon-14 synthesis was accomplished in six radiochemica...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Latli B,Eriksson M,Hrapchak M,Busacca CA,Senanayake CH

更新日期：2016-06-30 00:00:00

abstract：:MMP-9 is a zinc-dependent endopeptidase that is involved in the proteolytic degradation of the extracellular matrix and plays an important role in cancer migration, invasion, and metastasis. The aim of this study was to evaluate the potential of MMP-tracers [18 F]BR420 and [18 F]BR351 for MMP-9 imaging in a colorectal...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Vazquez N,Missault S,Vangestel C,Deleye S,Thomae D,Van der Veken P,Augustyns K,Staelens S,Dedeurwaerdere S,Wyffels L

更新日期：2017-01-01 00:00:00

abstract：:The syntheses of perdeuterated phytoalexins nasturlexins A and C, and putative biosynthetic precursors, including phenylethyl isothiocyanates and phenylethyl dithiocarbamates, using commercially available [2,3,4,5,6-D5 ]phenylalanine, [2,3,4,5,6-D5 ]nitrobenzene, and [2,3,4,5,6-D5 ]benzaldehyde are described. In addit...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Pedras MSC,To QH

更新日期：2018-02-01 00:00:00

abstract：:Dimethylsulfoniopropionate (DMSP, (2-carboxyethyl)dimethylsulfonium) is a highly abundant compound in marine environments. As a precursor to the climatically active gas, dimethylsulfide (DMS), DMSP connects the marine and terrestrial sulfur cycles. However, the fate of DMSP in microbial biomass is not well understood ...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Wirth JS,Whitman WB

更新日期：2019-01-01 00:00:00

abstract：:Targeted delivery of chemotherapeutic drug at the tumor site enhances the efficacy with minimum systemic exposure. Towards this, drugs conjugated with peptides having affinity towards a particular molecular target are recognized as affective agents for targeted chemotherapy. Thus, in the present study, tumor-homing as...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Vats K,Satpati D,Sharma R,Kumar C,Sarma HD,Dash A

更新日期：2017-07-01 00:00:00

abstract：:This study aimed to provide an easy method for synthesis of 1-hydroxy-2-(3-pyridyl) ethylidene bisphosphonic acid monosodium (sod. risedronate) with a high yield of 71%. The synthesized risedronate was labeled with technetium-99 m using two different reducing agents (SnCl2 .2H2 O and NaBH4 ) where NaBH4 gave stable co...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Motaleb MA,Adli AS,El-Tawoosy M,Sanad MH,AbdAllah M

更新日期：2016-04-01 00:00:00

abstract：:For the first time, [3α-(3) H] 17α-hydroxy pregnenolone (1) was synthesized through a multiple step sequence. The presence of [3β-(3) H] isomer in RP-HPLC purified product was identified by tritium NMR. The [3β-(3) H] isomer was then separated from [3α-(3) H] 17α-hydroxy pregnenolone with chiralPAK AD-H column. [3α-(3...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Tian Y,Hong Y,Bonacorsi SJ,Balog A,Gong S

更新日期：2014-01-01 00:00:00

abstract：:[18 F]DCFPyL is a clinical-stage PET radiotracer used to image prostate cancer. This report details the efficient production of [18 F]DCFPyL using single-step direct radiofluorination, without the use of carboxylic acid-protecting groups. Radiolabeling reaction optimization studies revealed an inverse correlation betw...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Dornan MH,Simard JM,Leblond A,Juneau D,Delouya G,Saad F,Ménard C,DaSilva JN

更新日期：2018-05-02 00:00:00

abstract：:As covalent modifiers of proteins, high-mannose N-glycans are important in maintaining protein structure and function in vivo. The conformations of these glycans can be studied by nuclear magnetic resonance spectroscopy using spin-spin couplings (J-couplings; scalar couplings) and other nuclear magnetic resonance para...

journal_title：Journal of labelled compounds & radiopharmaceuticals

authors： Zhang W,Pan Q,Serianni AS

更新日期：2016-12-01 00:00:00