- Preparation of Nonradioactive Standards and a Precursor for a Hypoxia 18 F PET Tracer Derived from 1-(β- d -Galactopyranosyl)-2-nitroimidazole
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Acetyl-protected 1-(β- d -galactopyranosyl)-2-nitroimidazole was converted to a potential precursor for a fluorine-18 labeled hypoxia tumor marker. Two nonradioactive standards, the 6′-deoxy-6′-fluorogalactosyl and the 4′-deoxy-4′-fluoroglucosyl analogue
- Schweifer, Anna,Malová Kri?ková, Petra,Mereiter, Kurt,Hammerschmidt, Friedrich
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Read Online
- Process development of selectively benzoylated and fluorinated glycosyl donors
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Route selection, process development and large-scale preparation of selectively benzoylated and fluorinated d-glucopyranoses, required as glycosyl donors for the synthesis of the SGLT inhibitor SAR7226, are discussed.
- Weiberth, Franz J.,Gill, Harpal S.,Jiang, Ying,Lee, George E.,Lienard, Philippe,Pemberton, Clive,Powers, Matthew R.,Subotkowski, Witold,Tomasik, Witold,Vanasse, Benoit J.,Yu, Yong
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p. 623 - 631
(2011/07/30)
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- METHOD FOR PRODUCING 4-DEOXY-4-FLUORO-D-GLUCOSE DERIVATIVE
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There is disclosed a method for producing a 4-deoxy-4-fluoro-D-glucose derivative by reacting a D-galactose derivative with either sulfuryl fluoride (SO2F2), trifluoromethanesulfonyl fluoride (CF3SO2F) or perflu
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Page/Page column 11-12
(2010/08/18)
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- Synthesis and structure elucidation of benzoylated deoxyfluoropyranosides
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Benzoylated deoxyfluoropyranosides have been synthesized, starting with protected, unprotected, or fluorinated precursors. Fluorination of eight derivatives was compared using DAST and Deoxo-Fluor as reagents. Deoxo-Fluor was found to be especially useful
- Esmurziev, Aslan M.,Simic, Nebojsa,Hoff, Bard Helge,Sundby, Eirik
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experimental part
p. 348 - 367
(2011/09/30)
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- Novel aromatic fluoroglycoside derivatives, medicaments containing these compounds, and the use thereof
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Novel aromatic fluoroglycoside derivatives, medicaments containing these compounds, and the use thereof. The invention relates to substituted aromatic fluoroglycoside derivatives of the formula I in which the radicals have the stated meanings, and their p
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Page/Page column 24-25
(2008/06/13)
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- NOVEL FLUOROGLYCOSIDE DERIVATIVES OF PYRAZOLES, MEDICAMENTS CONTAINING THESE COMPOUNDS, AND THE USE THEREOF
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The invention relates to substituted fluoroglycoside derivatives of pyrazoles of formula (I), in which the radicals have the indicated meanings, to the physiologically compatible salts thereof, and to a method for the production thereof. The compounds are suited for as, e.g. antidiabetics.
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Page/Page column 32-33
(2008/06/13)
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- NOVEL FLUOROGLYCOSIDE HETEROCYCLIC DERIVATIVES, PHARMACEUTICAL PRODUCTS CONTAINING SAID COMPOUNDS AND THE USE THEREOF
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The invention relates to substituted fluoroglycoside heterocyclic derivatives of a formula (I), wherein radicals have predefined bonds, to the psychologically tolerated salts thereof and to methods for the preparation thereof. Said compounds can be used, for example as antidiabetic agents.
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Page/Page column 39-40
(2008/06/13)
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- Synthesis of UDP-4-deoxy-4-fluoroglucose and UDP-4-deoxy-4-fluorogalactose and their interactions with enzymes of nucleotide sugar metabolism
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Fluorinated carbohydrates can be used as probes of enzymatic active sites. We report the synthesis of 4-deoxy-4-fluoro-α-D-galactose-1-phosphate and the substrate analogues of UDP-galactose, UDP4-deoxy-4-fluoro-α-D-galactose (UDP-FGal), and of UDP-glucose, UDP-4-deoxy-4-fluoro-α-D-glucose (UDP-FGlc), which may be useful in analyzing the binding properties of enzymes that utilize nucleotide sugars as substrates. As a first step in this study, we determine the kinetic and inhibition parameters for UDP-FGal and UDP-FGlc interacting with UDP-glucose dehydrogenase and UDP-galactose 4-epimerase. UDP-FGlc is a substrate for bovine liver UDP-glucose dehydrogenase: K(m) = 30.2 ± 4.5 μM slightly higher than the value 9.6 ± 0.7 μM for UDP-glucose, and V(m)(UDP-FGlc) = 0.46V(mUDP-Glc). UDP-FGal is not a substrate for UDP-glucose dehydrogenase but is a competitive inhibitor with respect to UDP-glucose (K(i) = 19.9 ± 6.6 μM). These analogs also bind to UDP-galactose 4-epimerase from E. coli with dissociation constants K(d) of 1.4 and 1.1 mM for UDP-FGlc and UDP-FGal, respectively.
- Chapeau,Frey
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p. 6994 - 6998
(2007/10/02)
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- THE SYNTHESIS AND HYDROLYSIS OF A SERIES OF DEOXYFLUORO-D-GLUCOPYRANOSYL PHOSPHATES
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The synthesis of all four deoxyfluoro-α-D-glucopyranosyl phosphates is described.Rate conctants for their acid-catalyzed hydrolysis were determined, and fluorine substitution was shown to have a significant effect in lowering the rate, particularly when t
- Withers, Stephen G.,MacLennan, David J.,Street, Ian P.
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p. 127 - 144
(2007/10/02)
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