4724-56-5Relevant articles and documents
Synthesis,18 F-Radiolabelling and Biological Characterization of Novel Fluoroalkylated Triazine Derivatives for in Vivo Imaging of Phosphodiesterase 2A in Brain via Positron Emission Tomography
Schr?der, Susann,Wenzel, Barbara,Deuther-Conrad, Winnie,Teodoro, Rodrigo,Egerland, Ute,Kranz, Mathias,Scheunemann, Matthias,H?fgen, Norbert,Steinbach, J?rg,Brust, Peter
, p. 9591 - 9615 (2015)
Phosphodiesterase 2A (PDE2A) is highly and specifically expressed in particular brain regions that are affected by neurological disorders and in certain tumors. Development of a specific PDE2A radioligand would enable molecular imaging of the PDE2A protei
New atropisomeric N-N ligands for CO/vinyl arene copolymerization reaction
Durand, Jerome,Zangrando, Ennio,Carfagna, Carla,Milani, Barbara
, p. 2171 - 2182 (2008)
New atropisomeric bidentate bipyridine-based ligands (3,3′- (ethylenedioxy)-2,2′-bipyridine 3; 3,3′-(propylenedioxy)-2,2′- bipyridine 4; 3,3′-(butylenedioxy)-2,2′-bipyridine 5) containing a bridge between the 3,3′ positions of the aromatic rings have been prepared. Together with the previously reported analogous ligands ((R)-3,3′-(1-methylethylenedioxy)-2,2′-bipyridine) 1 and ((S,S)-3,3′-(1,2-dimethylethylenedioxy)-2,2′-bipyridine) 2, they were used to synthesize the corresponding bis-chelated dicationic complexes [Pd(N-N)2][PF6]2. Crystal structures and comparison of the data obtained by X-ray analysis on four of these complexes is reported. These palladium compounds were used as precatalysts in the CO/styrene and CO/4-Me-styrene copolymerization reactions, where they showed that small variations in the ligand backbone remarkably affects the productivity of the catalytic system. The Royal Society of Chemistry 2008.
Macrocyclic compound, and preparation method and application thereof
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Paragraph 0209-0211, (2021/06/23)
The invention discloses a macrocyclic kinase inhibitor, and a compound, or a stereoisomer or a pharmaceutically acceptable salt thereof as shown in a formula (I). Experiments show that the novel compound shown in the formula (I) shows good TRK inhibitory
COMPOUNDS USEFUL IN HIV THERAPY
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Page/Page column 181; 182, (2020/06/19)
The invention relates to compounds of Formula (I), (Ia), (Ib), (II) or (III), salts thereof, pharmaceutical compositions thereof, as well as therapeutic methods of treatment and prevention.
Aggregation-induced emission based on a fluorinated macrocycle: visualizing spontaneous and ultrafast solid-state molecular motions at room temperature: via F?F interactions
Guo, Jingjing,He, Zhanyu,Irfan, Majeed,Liu, Tingting,Zeng, Zhuo,Zhang, Mei,Zhao, Zujin
supporting information, p. 14919 - 14924 (2020/11/17)
We for the first time report the efficient construction of novel tetraphenethylene (TPE)-based macrocycles with various mechanofluorochromism (MFC) behaviors involving solid-state molecular motions. We were able to facilely regulate the diverse solid-stat
Tetrastyrene macrocyclic compound with force-induced fluorescence color-changing performance and synthesis method and application thereof
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Paragraph 0059-0061, (2019/06/07)
The invention discloses a tetrastyrene macrocyclic compound with force-induced fluorescence color changing performance. The compound is connected with an alkyl chain structural unit through the strongfluorescence property of the tetrastyrene macrocyclic c
A compound for PET imaging and use thereof
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Paragraph 0068-0070, (2018/04/21)
The present invention provides a precursor compound for the production of a radioactive compound for efficient contrast of the heart, a radioactive compound prepared using the precursor compound, and uses as a contrast medium for a PET contrast medium.br
Synthesis, F-18 radiolabeling, and microPET evaluation of 3-(2,4-dichlorophenyl)-N-alkyl-N-fluoroalkyl-2,5-dimethylpyrazolo[1,5-a]pyrimidin-7-amines as ligands of the corticotropin-releasing factor type-1 (CRF1) receptor
Stehouwer, Jeffrey S.,Birnbaum, Matthew S.,Voll, Ronald J.,Owens, Michael J.,Plott, Susan J.,Bourke, Chase H.,Wassef, Michael A.,Kilts, Clinton D.,Goodman, Mark M.
, p. 4286 - 4302 (2015/08/03)
A series of 3-(2,4-dichlorophenyl)-N-alkyl-N-fluoroalkyl-2,5-dimethylpyrazolo[1,5-a]pyrimidin-7-amines were synthesized and evaluated as potential positron emission tomography (PET) tracers for the corticotropin-releasing factor type-1 (CRF1) receptor. Compounds 27, 28, 29, and 30 all displayed high binding affinity (≤1.2 nM) to the CRF1 receptor when assessed by in vitro competition binding assays at 23 °C, whereas a decrease in affinity (≥10-fold) was observed with compound 26. The log P7.4 values of [18F]26-[18F]29 were in the range of ~2.2-2.8 and microPET evaluation of [18F]26-[18F]29 in an anesthetized male cynomolgus monkey demonstrated brain penetrance, but specific binding was not sufficient enough to differentiate regions of high CRF1 receptor density from regions of low CRF1 receptor density. Radioactivity uptake in the skull, and sphenoid bone and/or sphenoid sinus during studies with [18F]28, [18F]28-d8, and [18F]29 was attributed to a combination of [18F]fluoride generated by metabolic defluorination of the radiotracer and binding of intact radiotracer to CRF1 receptors expressed on mast cells in the bone marrow. Uptake of [18F]26 and [18F]27 in the skull and sphenoid region was rapid but then steadily washed out which suggests that this behavior was the result of binding to CRF1 receptors expressed on mast cells in the bone marrow with no contribution from [18F]fluoride.
Synthesis and characterization of a novel series of agonist compounds as potential radiopharmaceuticals for imaging dopamine D2/3 receptors in their high-affinity state
Van Wieringen, Jan-Peter,Shalgunov, Vladimir,Janssen, Henk M.,Fransen, P. Michel,Janssen, Anton G. M.,Michel, Martin C.,Booij, Jan,Elsinga, Philip H.
, p. 391 - 410 (2014/02/14)
Imaging of dopamine D2/3 receptors (D2/3R) can shed light on the nature of several neuropsychiatric disorders in which dysregulation of D2/3R signaling is involved. Agonist D2/3 tracers for PET/SPECT imaging are considered to be superior to antagonists because they are more sensitive to dopamine concentrations and may selectively label the high-affinity receptor state. Carbon-11-labeled D2/3R agonists have been developed, but these short-lived tracers can be used only in centers with a cyclotron. Here, we report the development of a series of novel D2R agonist compounds based on the 2-aminomethylchromane (AMC) scaffold that provides ample opportunities for the introduction of longer-lived [ 18F] or [123I]. Binding experiments showed that several AMC compounds have a high affinity and selectivity for D2/3R and act as agonists. Two fluorine-containing compounds were [18F]-labeled, and both displayed specific binding to striatal D2/3R in rat brain slices in vitro. These findings encourage further in vivo evaluations.
Design and synthesis of polymeric chiral bicyclo[3.3.0] diene as reusable ligand for rhodium-catalyzed asymmetric 1,4-addition
Yang, Hongyu,Xu, Minghua
supporting information, p. 119 - 122 (2013/08/24)
A series of A-B type sterically regular bicyclio[3.3.0] diene-based polymers were designed and synthesized as immobilized chiral diene ligands for asymmetric catalysis. With polymeric diene 6b, good to excellent enantioselectivities can be achieved in Rh-catalyzed asymmetric 1,4-addition of arylboronic acids to α,β-unsaturated ketones. A series of A-B type sterically regular bicyclio[3.3.0] diene-based polymers were designed and synthesized as immobilized chiral diene ligands for asymmetric catalysis. By using polymeric diene, good to excellent enantioselectivities can be achieved in Rh-catalyzed asymmetric 1,4-addition of arylboronic acids to α,β-unsaturated ketones. Copyright