scholarly journals Optimized synthesis and indium complex formation with the bifunctional chelator NODIA-Me

2018 ◽  
Vol 16 (40) ◽  
pp. 7503-7512 ◽  
Author(s):  
Christian Weinmann ◽  
Jason P. Holland ◽  
Tilman Läppchen ◽  
Harald Scherer ◽  
Stephan Maus ◽  
...  
Keyword(s):  
Complex Formation ◽  
Radiochemical Purity ◽  
High Yield ◽  
Synthetic Route ◽  
Bifunctional Chelator ◽  
Indium Complex

Multi-step synthetic route provides the ligand NODIA-Me in high yield. Radiolabeling with [111In]InCl3 yields stable complexes in high radiochemical purity and yield.

scholarly journals A Synthetic Route to Quaternary Pyridinium Salt-Functionalized Silsesquioxanes

2012 ◽  
Vol 2012 ◽  
pp. 1-9 ◽  
Author(s):  
Nataliya Kostenko ◽  
Jochen Gottfriedsen ◽  
Liane Hilfert ◽  
Frank T. Edelmann
Keyword(s):  
Pyridinium Salt ◽  
High Yield ◽  
Synthetic Route ◽  
Alkylation Reactions ◽  
Partial Success

A synthetic route to potentially biocidal silsesquioxanes functionalized by quaternary pyridinium functionalities has been developed.N-Alkylation reactions of the precursor compounds 4-(2-(trimethoxysilyl)ethyl)-pyridine (5) and 4-(2-trichloro-silylethyl)pyridine (6) with iodomethane,n-hexylbromide, andn-hexadecylbromide cleanly afforded the correspondingN-alkylpyridinium salts (7–10). The synthesis of a 4-(2-ethyl)pyridine POSS derivative (2) was achieved by capping of the silsesquioxane trisilanol Cy7Si7O9(OH)3(1) via two different preparative routes. Attempts to use compound2as precursor for quaternary pyridinium salt-functionalized POSS derivatives were met with only partial success. Only the reaction with iodomethane cleanly afforded the newN-methylpyridinium salt12in high yield, whereasn-hexylbromide andn-hexadecylbromide failed to react with2even under forcing conditions.

In silico and in vivo study of radio-iodinated nefiracetam as a radiotracer for brain imaging in mice

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
M. H. Sanad ◽  
A. B. Farag ◽  
S. F. A. Rizvi
Keyword(s):  
Brain Imaging ◽  
Radiochemical Purity ◽  
High Yield ◽  
High Uptake ◽  
Oxidizing Agent ◽  
Receptor Ligand ◽  
Nootropic Agent ◽  
Biodistribution Studies

Abstract This study presents development and characterization of a radiotracer, [125I]iodonefiracetam ([125I]iodoNEF). Labeling with high yield and radiochemical purity was achieved through the formation of a [125I]iodoNEF radiotracer after investigating many factors like oxidizing agent content (chloramines-T (Ch-T)), substrate amount (Nefiracetam (NEF)), pH of reaction mixture, reaction time and temperature. Nefiracetam (NEF) is known as nootropic agent, acting as N-methyl-d-aspartic acid receptor ligand (NMDA). The radiolabeled compound was stable, and exhibited the logarithm of the partition coefficient (log p) value of [125I]iodonefiracetam as 1.85 (lipophilic). Biodistribution studies in normal mice confirmed the suitability of the [125I]iodoNEF radiotracer as a novel tracer for brain imaging. High uptake of 8.61 ± 0.14 percent injected dose/g organ was observed in mice

scholarly journals Multi-curie production of gallium-68 on a biomedical cyclotron and automated radiolabelling of PSMA-11 and DOTATATE

2021 ◽  
Vol 6 (1) ◽  
Author(s):  
Helge Thisgaard ◽  
Joel Kumlin ◽  
Niels Langkjær ◽  
Jansen Chua ◽  
Brian Hook ◽  
...  
Keyword(s):  
Radiochemical Purity ◽  
High Yield ◽  
Clinical Use ◽  
Automated Production ◽  
Automated Method ◽  
Gallium 68 ◽  
High Yields ◽  
High Level ◽  
Mev Protons ◽  
Very High

Abstract Background With increasing clinical demand for gallium-68, commercial germanium-68/gallium-68 ([68Ge]Ge/[68Ga]Ga) generators are incapable of supplying sufficient amounts of the short-lived daughter isotope. In this study, we demonstrate a high-yield, automated method for producing multi-Curie levels of [68Ga]GaCl3 from solid zinc-68 targets and subsequent labelling to produce clinical-grade [68Ga]Ga-PSMA-11 and [68Ga]Ga-DOTATATE. Results Enriched zinc-68 targets were irradiated at up to 80 µA with 13 MeV protons for 120 min; repeatedly producing up to 194 GBq (5.24 Ci) of purified gallium-68 in the form of [68Ga]GaCl3 at the end of purification (EOP) from an expected > 370 GBq (> 10 Ci) at end of bombardment. A fully automated dissolution/separation process was completed in 35 min. Isolated product was analysed according to the Ph. Eur. monograph for accelerator produced [68Ga]GaCl3 and found to comply with all specifications. In every instance, the radiochemical purity exceeded 99.9% and importantly, the radionuclidic purity was sufficient to allow for a shelf-life of up to 7 h based on this metric alone. Fully automated production of up to 72.2 GBq [68Ga]Ga-PSMA-11 was performed, providing a product with high radiochemical purity (> 98.2%) and very high apparent molar activities of up to 722 MBq/nmol. Further, manual radiolabelling of up to 3.2 GBq DOTATATE was performed in high yields (> 95%) and with apparent molar activities (9–25 MBq/nmol) sufficient for clinical use. Conclusions We have developed a high-yielding, automated method for the production of very high amounts of [68Ga]GaCl3, sufficient to supply proximal radiopharmacies. The reported method led to record-high purified gallium-68 activities (194 GBq at end of purification) and subsequent labelling of PSMA-11 and DOTATATE. The process was highly automated from irradiation through to formulation of the product, and as such comprised a high level of radiation protection. The quality control results obtained for both [68Ga]GaCl3 for radiolabelling and [68Ga]Ga-PSMA-11 are promising for clinical use.

Synthesis, Processing and Phase Evolution of TiN/TiB2 Composites From Polymeric Precursors

1992 ◽  
Vol 286 ◽  
Author(s):  
M. Nowakowski ◽  
K. Su ◽  
L. Sneddon ◽  
D. Bonnell
Keyword(s):  
Phase Evolution ◽  
High Yield ◽  
Microstructural Development ◽  
Synthetic Route ◽  
Polymeric Precursors

ABSTRACTA high yield synthetic route to TiN/TiB2 nanocomposites based upon polymeric precursors has been developed. The phase evolution and microstructural development have been characterized and related to preliminary measurements of properties, i.e. hardness. The observations indicate the existence of TiN-TiB2, TiN-BN, and TiB2-BN subsolidus compatibilities.

scholarly journals Full N,N-Methylation of 4,4′-Methylenedianiline with Dimethyl Carbonate: A Feasible Access to 4,4′-Methylene bis(N,N-Dimethylaniline)

2018 ◽  
Vol 2018 ◽  
pp. 1-10
Author(s):  
Zegang Qiu ◽  
Kunjie Wang ◽  
Zhiqin Li ◽  
Tao Li ◽  
Jinhao Bai ◽  
...  
Keyword(s):  
Zinc Acetate ◽  
Dimethyl Carbonate ◽  
Reaction Pathway ◽  
Major Product ◽  
High Yield ◽  
Synthetic Route ◽  
Reaction Conditions ◽  
High Yields ◽  
By Products

The full N,N-methylation of 4,4′-methylenedianiline (MDA) with dimethyl carbonate (DMC) was investigated. The yield of the major product 4,4′-methylene bis(N,N-dimethylaniline) (MBDMA) reached as high as 97% over NaY catalyst at 190°C for 6 h. The catalyst could be used for two more times with acceptable MBDMA yields higher than 90%. The main by-products were identified as three N-methylated derivatives. Surprisingly, the formation of the N-methoxycarbonylation product was extremely restrained, which could be produced in high yields of 98% on zinc acetate catalyst. Furthermore, the reaction pathway to the major product MBDMA was proposed. Finally, a feasible synthetic route of 4,4′-methylene bis(N,N-dimethylaniline) (MBDMA) was established, featuring a high yield, mild reaction conditions, and simple operations.

scholarly journals Multi-Curie Production of Gallium-68 on a Biomedical Cyclotron and Automated Radiolabelling of PSMA-11 and DOTATATE

2020 ◽  
Author(s):  
Helge Thisgaard ◽  
Joel Kumlin ◽  
Niels Langkjær ◽  
Jansen Chua ◽  
Brian Hook ◽  
...  
Keyword(s):  
Radiochemical Purity ◽  
High Yield ◽  
Clinical Use ◽  
Automated Production ◽  
Automated Method ◽  
Gallium 68 ◽  
High Yields ◽  
High Level ◽  
Mev Protons ◽  
Very High

Abstract Background: With increasing clinical demand for gallium-68, commercial germanium-68/gallium-68 ([68Ge]Ge/[68Ga]Ga) generators are incapable of supplying sufficient amounts of the short-lived daughter isotope. In this study, we demonstrate a high-yield, automated method for producing multi-Curie levels of [68Ga]GaCl3 from solid zinc-68 targets and subsequent labelling to produce clinical-grade [68Ga]Ga-PSMA-11 and [68Ga]Ga-DOTATATE.Results: Enriched zinc-68 targets were irradiated at up to 80 µA with 13 MeV protons for 120 min; repeatedly producing up to 194 GBq (5.24 Ci) of purified gallium-68 in the form of [68Ga]GaCl3 at the end of purification (EOP) from an expected >370 GBq (>10 Ci) at end of bombardment. A fully automated dissolution/separation process was completed in 35 min. Isolated product was analysed according to the draft Ph. Eur. monograph for accelerator produced [68Ga]GaCl3 and found to comply with all specifications. In every instance, the radiochemical purity exceeded 99.9% and importantly, the radionuclidic purity was sufficient to allow for a shelf-life of up to 7 h based on this metric alone. Fully automated production of up to 72.2 GBq [68Ga]Ga-PSMA-11 was performed, providing a product with high radiochemical purity (>98.2%) and very high apparent molar activities of up to 722 MBq/nmol. Further, manual radiolabelling of up to 3.2 GBq DOTATATE was performed in high yields (>95%) and with apparent molar activities (9-25 MBq/nmol) sufficient for clinical use.Conclusions: We have developed a high-yielding, automated method for the production of very high amounts of [68Ga]GaCl3, sufficient for supply proximal radiopharmacies. The reported method led to record-high purified gallium-68 activities (194 GBq at end of purification) and subsequent labelling of PSMA-11 and DOTATATE. The process was highly automated from irradiation through to formulation of the product, and as such comprised a high level of radiation protection. The quality control results obtained for both [68Ga]GaCl3 for radiolabelling and [68Ga]Ga-PSMA-11 are promising for clinical use.

Facile Synthetic Route for Direct Access of Perylenediimide Single Crystals in High Yield through In Situ Crystallization

2020 ◽  
Vol 5 (6) ◽  
pp. 2070-2074
Author(s):  
Jayaraman Pitchaimani ◽  
Anu Kundu ◽  
Savarimuthu Philip Anthony ◽  
Dohyun Moon ◽  
Vedichi Madhu
Keyword(s):  
Single Crystals ◽  
Direct Access ◽  
High Yield ◽  
Synthetic Route ◽  
In Situ Crystallization

scholarly journals Synthesis and Intramolecular Energy- and Electron-Transfer of 3D-Conformeric Tris(fluorenyl-[60]fullerenylfluorene) Derivatives

Molecules ◽  
2019 ◽  
Vol 24 (18) ◽  
pp. 3337
Author(s):  
He Yin ◽  
Min Wang ◽  
Loon-Seng Tan ◽  
Long Y. Chiang
Keyword(s):  
Electron Transfer ◽  
Direct Contact ◽  
Photophysical Properties ◽  
Molecular Packing ◽  
The Self ◽  
High Yield ◽  
Synthetic Route ◽  
Quenching Effect ◽  
Shape Structure ◽  
Energy And Electron Transfer

New 3D conformers were synthesized to show a nanomolecular configuration with geometrically branched 2-diphenylaminofluorene (DPAF-C2M) chromophores using a symmetrical 1,3,5-triaminobenzene ring as the center core for the connection of three fused DPAF-C2M moieties. The design led to a class of cis-cup-tris[(DPAF-C2M)-C60(>DPAF-C9)] 3D conformers with three bisadduct-analogous <C60> cages per nanomolecule facing at the same side of the geometrical molecular cis-cup-shape structure. A sequential synthetic route was described to afford this 3D configurated conformer in a high yield with various spectroscopic characterizations. In principle, a nanostructure with a non-coplanar 3D configuration in design should minimize the direct contact or π-stacking of fluorene rings with each other during molecular packing to the formation of fullerosome array. It may also prevent the self-quenching effect of its photoexcited states in solids. Photophysical properties of this cis-cup-conformer were also investigated.

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