Journal of labelled compounds & radiopharmaceuticals最新文献_第8页

Luminescence enhancement by deuterium 氘的发光增强。

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2023-08-16 DOI: 10.1002/jlcr.4056

Crist N. Filer

引用次数: 0

Enzymatic synthesis of halogen derivatives of L-phenylalanine and phenylpyruvic acid stereoselectively labeled with hydrogen isotopes in the side chain 酶法合成L-苯丙氨酸和苯基丙酮酸的卤素衍生物，在侧链中用氢同位素立体标记。

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2023-08-02 DOI: 10.1002/jlcr.4057

Katarzyna Pałka, Katarzyna Podsadni, Małgorzata Pająk

引用次数: 1

Carbon 14 and stable isotope synthesis of two potent and selective phosphodiesterase type 4 inhibitors 碳14和两种强效选择性磷酸二酯酶4型抑制剂的稳定同位素合成。

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2023-07-24 DOI: 10.1002/jlcr.4054

Bachir Latli, Matt J. Hrapchak, Thomas G. Tampone, Rogelio P. Frutos, Heewon Lee

{"title":"Carbon 14 and stable isotope synthesis of two potent and selective phosphodiesterase type 4 inhibitors","authors":"Bachir Latli, Matt J. Hrapchak, Thomas G. Tampone, Rogelio P. Frutos, Heewon Lee","doi":"10.1002/jlcr.4054","DOIUrl":"10.1002/jlcr.4054","url":null,"abstract":"(R)-2-(4-(Benzo[d]oxazol-2-yl)piperazin-1-yl)-4-((tetrahydro-2H-pyran-4-yl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (1) and (R)-2-(4-(4-chlorophenoxy)piperidin-1-yl)-4-((tetrahydro-2H-pyran-4-yl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (2) are two potent and selective inhibitors of phosphodiesterase type 4 (PDE4). In this manuscript, we report the detailed synthesis of these two compounds labeled with carbon 14 and with stable isotopes. The core (R)-4-((tetrahydro-2H-pyran-4-yl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide is common in both inhibitors. In the radioactive synthesis, the carbon 14 atom was introduced in the benzoxazole moiety using [14C]carbon disulfide to obtain [14C]-1 in five steps at a 55% overall yield. [14C]Urea was used to incorporate the carbon 14 atom in two steps in the dihydrothieno[3,2-d]pyrimidine intermediate, which was then transformed in four more steps to [14C]-2 at a 30% overall yield. Both compounds were isolated with specific activities higher than 54 mCi/mmol, radio- and chemical-purities higher than 99%, and with excellent enantiomeric excess. In the stable isotope synthesis, [2H8]piperazine was used to prepare [2H8]-1 in three steps in 72% overall yield, while [13C6]phenol was used to prepare [13C6]-2 in four steps in 18% overall yield.","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"66 11","pages":"353-361"},"PeriodicalIF":1.8,"publicationDate":"2023-07-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10205849","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 approach to the optimization of positron emission tomography imaging agents for the central nervous system 一种实用的方法来优化正电子发射断层成像剂的中枢神经系统

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2023-07-20 DOI: 10.1002/jlcr.4047

引用次数: 0

Featured Cover 特色封面

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2023-07-20 DOI: 10.1002/jlcr.4055

引用次数: 0

Development of an economical method to synthesize O-(2-[18F]fluoroethyl)-L-tyrosine (18FFET) 经济合成O-（2-[18F]氟乙基）-L-酪氨酸（18FFET）方法的研究

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2023-07-06 DOI: 10.1002/jlcr.4052

Aishwarya Kumar, Raman Kumar Joshi, Riptee Thakur, Dinesh Kumar, Chandana Nagaraj, Pardeep Kumar

{"title":"Development of an economical method to synthesize O-(2-[18F]fluoroethyl)-L-tyrosine (18FFET)","authors":"Aishwarya Kumar, Raman Kumar Joshi, Riptee Thakur, Dinesh Kumar, Chandana Nagaraj, Pardeep Kumar","doi":"10.1002/jlcr.4052","DOIUrl":"https://doi.org/10.1002/jlcr.4052","url":null,"abstract":"Positron emission tomography (PET) using O-(2-[18F]fluoroethyl)-L-tyrosine ([18F]FET) has shown great success in differentiating tumor recurrence from necrosis. In this study, we are reporting the experience of synthesis [18F]FET by varying the concentration of TET precursor in different chemistry modules. TET precursor (2–10 mg) was used for the synthesis of [18F]FET in an automated (MX Tracerlab) module (n = 6) and semiautomated (FX2N Tracerlab) module (n = 19). The quality control was performed for all the preparations. For human imaging, 220 ± 50 MBq of [18F]FET was briefly injected into the patient to acquire PET-MR images. The radiochemical purity was greater than 95% for the final product in both modules. The decay corrected average yield was 10.7 ± 4.7% (10 mg, n = 3) and 8.2 ± 2.6% (2 mg, n = 3) with automated chemistry module and 36.7 ± 7.3% (8–10 mg, n = 12), 26.4 ± 3.1% (5–7 mg, n = 4), and 35.1 ± 3.8% (2–4 mg, n = 3) with semiautomated chemistry modules. The PET imaging showed uptake at the lesion site (SUVmax = 7.5 ± 2.6) and concordance with the MR image. The [18F]FET was produced with a higher radiochemical yield with 2.0 mg of the precursor with substantial yield and is suitable for brain tumor imaging.","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"66 11","pages":"345-352"},"PeriodicalIF":1.8,"publicationDate":"2023-07-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"50133328","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

Blood Brain Barrier – tactics and attributes in developing successful neuroimaging agents 血脑屏障-开发成功的神经成像剂的策略和属性。

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2023-07-06 DOI: 10.1002/jlcr.4053

Selena Milicevic Sephton, Stephen Thompson

引用次数: 0

Carbon 14 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）的碳14合成及其主要代谢产物。

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2023-06-29 DOI: 10.1002/jlcr.4051

Bachir Latli, Matt J. Hrapchak, Rogelio P. Frutos, Heewon Lee, Jinhua J. Song

{"title":"Carbon 14 synthesis of glycine transporter 1 inhibitor Iclepertin (BI 425809) and its major metabolites","authors":"Bachir Latli, Matt J. Hrapchak, Rogelio P. Frutos, Heewon Lee, Jinhua J. Song","doi":"10.1002/jlcr.4051","DOIUrl":"10.1002/jlcr.4051","url":null,"abstract":"Carbon 14 labeled Iclepertin (BI 425809, 1) and its major metabolites were needed for ADME and several other studies necessary for the advancement of this drug candidate in clinical trials. Iclepertin is composed of two main chemical blocks, (R)-5-(methylsulfonyl)-2-([1,1,1-trifluoropropan-2-yl]oxy)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. In the first synthesis of carbon 14 labeled 1, 2-fluorobenzoic acid, carboxyl-14C was converted to [14C]-2 in three steps and then coupled to 3 to provide [14C]-1a in 45% overall yield. In the second synthesis, [14C]-3 was prepared in six radioactive steps and coupled to the acid 2 to furnish [14C]-1b in 20% overall yield. Both synthetic routes provided [14C]-1a and [14C]-1b with specific activities higher than 53 mCi/mmol and radiochemical, chemical, and enantiomeric purities above 98%. Two major metabolites of 1, BI 761036 and BI 758790, were also prepared labeled with carbon 14 using intermediates already available from the synthesis of [14C]-1.","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"66 11","pages":"336-344"},"PeriodicalIF":1.8,"publicationDate":"2023-06-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10206831","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

Mild and selective hydrogen–deuterium exchange for aromatic hydrogen of amines 温和和选择性的氢-氘交换胺的芳香族氢

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2023-06-19 DOI: 10.1002/jlcr.4048

Zetryana Puteri Tachrim, Manami Hashinoki, Zeping Wang, Zhang Wen, Zhuang Zihan, Makoto Hashimoto

引用次数: 0

Applications of radiolabeled antibodies in neuroscience and neuro-oncology 放射性标记抗体在神经科学和神经肿瘤学中的应用。

IF 1.8 4区医学

Journal of labelled compounds & radiopharmaceuticals Pub Date : 2023-06-15 DOI: 10.1002/jlcr.4049

Ryan J. Pakula, Peter J. H. Scott

引用次数: 0