54154-11-9Relevant academic research and scientific papers
Asymmetric Transfer Hydrogenation of α-Keto Amides; Highly Enantioselective Formation of Malic Acid Diamides and α-Hydroxyamides
Gediya, Shweta K.,Vyas, Vijyesh K.,Clarkson, Guy J.,Wills, Martin
supporting information, p. 7803 - 7807 (2021/10/20)
The asymmetric transfer hydrogenation (ATH) of α-keto-1,4-diamides using a tethered Ru/TsDPEN catalyst was achieved in high ee. Studies on derivatives identified the structural elements which lead to the highest enantioselectivities in the products. The α-keto-amide reduction products have been converted to a range of synthetically valuable derivatives.
Copper-Catalysed (Diacetoxyiodo)benzene-Promoted Aerobic Esterification Reaction: Synthesis of Oxamates from Acetoacetamides
Zhang, Zhiguo,Gao, Xiaolong,Yu, Haifeng,Zhang, Guisheng,Liu, Jianming
supporting information, p. 3406 - 3411 (2018/07/31)
A copper-catalysed (diacetoxyiodo)benzene-promoted aerobic esterification reaction of acetoacetamides was developed for the synthesis of oxamates, which are useful precursors in synthetic organic chemistry. This practical and mild synthetic approach proceeded at 25 °C under open-air conditions and afforded methyl 2-oxo-2-(phenylamino)acetates in good to excellent yields combined with C?C σ-bond cleavage and formal oxidative C?H bond functionalization. A mechanism is proposed. (Figure presented.).
Dibutyltin oxide catalyzed aminolysis of oxalate to carbamate, oxamate and derivatives of imidazolidine trione
Kunde, Lalita B.,Kalyani, Vishwanath S.,Gupte, Sunil P.
experimental part, p. 402 - 407 (2010/08/06)
Catalytic aminolysis of oxalates by simple and substituted ureas has been shown to give carbamates, oxamates and derivatives of imidazolidine trione. Various substituted ureas and oxalates were screened to verify the applicability of the protocol. The rol
Characterization of oxalic acid derivatives as new metabolites of metamizol (dipyrone) in incubated hen's egg and human
Wessel, Julia C.,Matyja, Magdalena,Neugebauer, Michael,Kiefer, Heiko,Daldrup, Thomas,Tarbah, Fuad A.,Weber, Horst
, p. 15 - 25 (2007/10/03)
Metamizol (dipyrone, 1), a widely used drug with effective analgesic and antispasmodic properties, shows severe side effects like agranulocytosis and anaphylactic shock reactions, the reasons of which are not known until today. After oral administration 1
RAF MODULATORS AND METHODS OF USE
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Page/Page column 70, (2010/02/14)
The present invention relates to compounds of the Formula I, wherein G, A, X1, X2, X3, Z, E, Y, and X are defined herein. The compounds modulate protein kinase enzymatic activity to modulate cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly Raf. Methods of using and preparing the compounds, and pharmaceutical compositions thereof, to treat kinase-dependent diseases and conditions are also an aspect of the invention.
Oxamyl dipeptide caspase inhibitors developed for the treatment of stroke
Linton, Steven D.,Aja, Teresa,Allegrini, Peter R.,Deckwerth, Thomas L.,Diaz, Jose-Luis,Hengerer, Bastian,Herrmann, Julia,Jahangiri, Kathy G.,Kallen, Joerg,Karanewsky, Donald S.,Meduna, Steven P.,Nalley, Kip,Robinson, Edward D.,Roggo, Silvio,Rovelli, Giorgio,Sauter, Andre,Sayers, Robert O.,Schmitz, Albert,Smidt, Robert,Ternansky, Robert J.,Tomaselli, Kevin J.,Ullman, Brett R.,Wiessner, Christoph,Wu, Joe C.
, p. 2685 - 2691 (2007/10/03)
Structural modifications were made to a previously described acyl dipeptide caspase inhibitor, leading to the oxamyl dipeptide series. Subsequent SAR studies directed toward the warhead, P2, and P4 regions of this novel peptidomimetic are described herein.
3-Hydroxy-quinolin-2-ones: Inhibitors of [3H]-glycine binding to the site associated with the NMDA receptor
Sit, Sing-Yuen,Ehrgott, Frederick J.,Gao, Jinnian,Meanwell, Nicholas A.
, p. 499 - 504 (2007/10/03)
A series of substituted 3-hydroxy-quinolin-2-one derivatives 6 was synthesized and evaluated as inhibitors of [3H]-glycine and [3H]-AMPA binding to rat cortical membranes. These compounds were generally found to be more potent ligands for the NMDA-associated glycine binding site than the AMPA receptor. Affinity for the glycine site was found to be influenced by both the electronic and steric properties associated with the C-4 substituent and the nature and pattern of substitution of the aromatic ring. The most active compound in this series, 6y, displaces [3H]-glycine with an IC50 of 29 nM.
Ring-Transformationen bei der Umsetzung von 3-(Dimethylamino)-2,2-dimethyl-2H-azirin mit 1-substituierten Imidazolidin-2,4,5-trionen
Schlaepfer-Daehler, Marlise,Heimgartner, Heinz
, p. 2321 - 2328 (2007/10/02)
Reaction of 1-substituted imidazolidine-2,4,5-triones ( = N-substituted parabanic acids; 2) and 3-(dimethylamino)-2,2-dimethyl-2H-azirine (1) in i-PrOH or MeCN at room temperature yields 5,6,7,7a-tetrahydro-3H-imidazoimidazole-5,7-diones 3 (Scheme
Cyclols as Intermediates in the Reaction of 3-(Dimethylamino)-2,2-dimethyl-2H-azirine with Monosubstituted Parabanic Acids; a New and Unexpected Rearrangement
Daehler, Marlise,Prewo, Roland,Bieri, Jost H.,Heimgartner, Heinz
, p. 1456 - 1465 (2007/10/02)
The reaction of 3-(dimethylamino)-2,2-dimethyl-2H-azirine (1) with N-methylparabanic acid (4) in 2-propanol at room temperature gives the cyclol 5 in 97 percent yield.In acetonitrile solution 5 rearranges to the imidazoline derivative 6 (Scheme 2).The str
