1358778-98-9Relevant academic research and scientific papers
Derisking the Cu-Mediated 18F-Fluorination of Heterocyclic Positron Emission Tomography Radioligands
Taylor, Nicholas J.,Emer, Enrico,Preshlock, Sean,Schedler, Michael,Tredwell, Matthew,Verhoog, Stefan,Mercier, Joel,Genicot, Christophe,Gouverneur, Véronique
, p. 8267 - 8276 (2017/06/27)
Molecules labeled with fluorine-18 (18F) are used in positron emission tomography to visualize, characterize and measure biological processes in the body. Despite recent advances in the incorporation of 18F onto arenes, the development of general and efficient approaches to label radioligands necessary for drug discovery programs remains a significant task. This full account describes a derisking approach toward the radiosynthesis of heterocyclic positron emission tomography (PET) radioligands using the copper-mediated 18F-fluorination of aryl boron reagents with 18F-fluoride as a model reaction. This approach is based on a study examining how the presence of heterocycles commonly used in drug development affects the efficiency of 18F-fluorination for a representative aryl boron reagent, and on the labeling of more than 50 (hetero)aryl boronic esters. This set of data allows for the application of this derisking strategy to the successful radiosynthesis of seven structurally complex pharmaceutically relevant heterocycle-containing molecules.
ELECTRON TRANSPORT MATERIAL AND ORGANIC ELECTROLUMINESCENT DEVICE USING SAME
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, (2016/10/08)
The invention concerns a compound represented by formula (1) below, and an organic EL device using the same. The compound of the invention is useful as an electron transport material that contributes to improvement in service life prolongation, reduction of driving voltage, achievement of high efficiency and so forth, above all, improvement in achieving high efficiency, and can provide an excellent organic EL device: wherein, Ar is an m-valent group derived from aromatic hydrocarbon or an aromatic heterocycle; X1 to X6 are ═CR1— or ═N—, at least two of X1 to X6 is ═CR1—, R1 in two of ═CR1— is a bonding hand to be bonded with Ar or an azole ring, and R1 in ═CR1— other than the above is hydrogen or alkyl having 1 to 4 carbons; Y is —O— or —S—; at least one of hydrogen in an azole ring may be replaced by alkyl, phenyl or naphthyl; m is an integer from 2 to 4; and at least one of hydrogen in each ring and alkyl in the formula may be replaced by deuterium.
Pyridone methylsulfone hydroxamate LpxC inhibitors for the treatment of serious Gram-negative infections
Montgomery, Justin I.,Brown, Matthew F.,Reilly, Usa,Price, Loren M.,Abramite, Joseph A.,Arcari, Joel,Barham, Rose,Che, Ye,Chen, Jinshan Michael,Chung, Seung Won,Collantes, Elizabeth M.,Desbonnet, Charlene,Doroski, Matthew,Doty, Jonathan,Engtrakul, Juntyma J.,Harris, Thomas M.,Huband, Michael,Knafels, John D.,Leach, Karen L.,Liu, Shenping,Marfat, Anthony,McAllister, Laura,McElroy, Eric,Menard, Carol A.,Mitton-Fry, Mark,Mullins, Lisa,Noe, Mark C.,O'Donnell, John,Oliver, Robert,Penzien, Joseph,Plummer, Mark,Shanmugasundaram, Veerabahu,Thoma, Christy,Tomaras, Andrew P.,Uccello, Daniel P.,Vaz, Alfin,Wishka, Donn G.
supporting information; experimental part, p. 1662 - 1670 (2012/04/17)
The synthesis and biological activity of a new series of LpxC inhibitors represented by pyridone methylsulfone hydroxamate 2a is presented. Members of this series have improved solubility and free fraction when compared to compounds in the previously described biphenyl methylsulfone hydroxamate series, and they maintain superior Gram-negative antibacterial activity to comparator agents.
