1208004-82-3Relevant academic research and scientific papers
Deoxyfluorination with CuF2: Enabled by Using a Lewis Base Activating Group
Bode, Bela E.,Chabbra, Sonia,Champion, Sue,Dawson, Daniel M.,Sood, D. Eilidh,Sutherland, Andrew,Watson, Allan J. B.
supporting information, p. 8460 - 8463 (2020/04/10)
Deoxyfluorination is a primary method for the formation of C?F bonds. Bespoke reagents are commonly used because of issues associated with the low reactivity of metal fluorides. Reported here is the development of a simple strategy for deoxyfluorination, using first-row transition-metal fluorides, and it overcomes these limitations. Using CuF2 as an exemplar, activation of an O-alkylisourea adduct, formed in situ, allows effective nucleophilic fluoride transfer to a range of primary and secondary alcohols. Spectroscopic investigations have been used to probe the origin of the enhanced reactivity of CuF2. The utility of the process in enabling 18F-radiolabeling is also presented.
Chiral phosphoric acid catalyzed enantioselective [4 + 2] cycloaddition reaction of α-fluorostyrenes with imines
Terada, Masahiro,Kikuchi, Jun,Ye, Haiting
supporting information, p. 8957 - 8961 (2020/12/02)
An enantioselective [4 + 2] cycloaddition reaction of α-fluorostyrenes with N-benzoyl imines was demonstrated using a chiral phosphoric acid catalyst. Cycloaddition products having fluorine functionality were formed in high yields with excellent diastereo
Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HT2C) receptor agonist without 5-HT2B agonism
Cheng, Jianjun,Kozikowski, Alan P.,McCorvy, John D.,Roth, Bryan L.,Shen, Sida,Zhang, Guiping
supporting information, (2019/08/26)
A new series of fluorinated 5-HT2C agonists were designed and synthesized on the basis of our previous work on 2-phenylcyclopropylmethylamines as a potential approach for the treatment of central nervous system disorders. Key fluorinated cyclop
Potent and Selective Neuronal Nitric Oxide Synthase Inhibitors with Improved Membrane Permeability
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, (2010/08/07)
Compounds and related compositions and methods as can be used to inhibit neuronal nitric oxide synthase and as can be employed in the treatment of various neurodegenerative diseases.
Potent and selective neuronal nitric oxide synthase inhibitors with improved cellular permeability
Xue, Fengtian,Fang, Jianguo,Lewis, William W.,Martasek, Pavel,Roman, Linda J.,Silverman, Richard B.
supporting information; experimental part, p. 554 - 557 (2010/04/26)
Recently, a series of potent and selective neuronal nitric oxide synthase inhibitors containing two basic nitrogen atoms was reported (Ji, H.; Stanton, B. Z.; Igarashi, J.; Li, H.; Martasek, P.; Roman, L. J.; Poulos, T. L.; Silverman, R. B. J. Am. Chem. Soc. 2008, 130, 3900-3914). In an effort to improve their bioavailability, three compounds (2a-c) were designed with electron-withdrawing groups near one of the basic nitrogen atoms to lower its pKa. Inhibition studies with these compounds showed that two of them not only retained most of the potency and selectivity of the best analogue of the earlier series, but also showed improved membrane permeability based on data from a cell-based assay.
POTENT AND SELECTIVE NEURONAL NITRIC OXIDE SYNTHASE INHIBITORS WITH IMPROVED MEMBRANE PERMEABILITY
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Page/Page column 35-36, (2010/08/08)
Compounds and related compositions and methods as can be used to inhibit neuronal nitric oxide synthase and as can be employed in the treatment of various neurodegenerative diseases.
