1515-85-1Relevant articles and documents
Reaction of phosphonium ylides and aromatic nitriles under lewis acid conditions: An easy access to aryl-substituted α-methoxyacetophenones
Camuzat-Dedenis,Provot,Moskowitz,Mayrargue
, p. 1558 - 1560 (1999)
In the presence of lithium chloride, as Lewis acid, the reaction of methoxymethyltriphenylphosphonium ylide 1 with aromatic nitriles 2 as phenacyl cation equivalents gives access to the corresponding α- methoxyacetophenones 3 in good yields.
SMALL MOLECULE ACTIVATORS OF NICOTINAMIDE PHOSPHORIBOSYLTRANSFERASE (NAMPT) AND USES THEREOF
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, (2018/08/03)
Provided herein are small molecule activators of Nicotinamide Phosphoribosyltransferase (NAMPT), compositions comprising the compounds, and methods of using the compounds and compositions.
Visible-Light-Mediated Aromatic Substitution Reactions of Cyanoarenes with 4-Alkyl-1,4-dihydropyridines through Double Carbon-Carbon Bond Cleavage
Nakajima, Kazunari,Nojima, Sunao,Sakata, Ken,Nishibayashi, Yoshiaki
, p. 1028 - 1032 (2016/04/05)
Novel aromatic substitution reactions of cyanoarenes with 4-alkyl-1,4-dihydropyridines as alkylating reagents in the presence of a catalytic amount of a photoredox catalyst proceed smoothly to give the corresponding alkyl-substituted arenes in good to high yields. The present reaction system realizes a novel C-C bond-forming reaction between two fragments generated from the C-C bond-cleavage reactions of two independent substrates.
Environmentally benign metal triflate-catalyzed reductive cleavage of the C-O bond of acetals to ethers
Zhang, Yin-Jie,Dayoub, Wissam,Chen, Guo-Rong,Lemaire, Marc
experimental part, p. 2737 - 2742 (2011/11/29)
A protocol is described for the reductive cleavage of the C-O bond of aromatic and aliphatic acetals to ethers catalyzed by Cu(OTf)2 or Bi(OTf)3 at room temperature in excellent yields, without affecting aromatic rings, nitro, nitrile, ester and hydroxyl groups. This protocol represents an improvement in terms of atom economy compared to the previous methods, by distinctly decreasing the amount of the reducing reagent, 1,1,3,3-tetramethyldisiloxane (TMDS), and using a small amount of catalyst.
1,2,4-TRIAZINE-4-AMINE DERIVATIVES
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Page/Page column 94-95, (2011/09/14)
According to the invention there is provided a compound of formula A1 which may be useful in the treatment of a condition or disorder ameliorated by the inhibition of the A1- A2b or, particularly, the A2a receptor wherein the compound of formula A1 has the structure, wherein, A represents Cy1 or HetA; Cy1 represents a 5- to 14-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one, two or three rings, which Cy1 group is optionally substituted by one or more R4a substituents; HetA represents a 5- to 14-membered heterocyclic group that may be aromatic, fully saturated or partially unsaturated, and which contains one or more heteroatoms selected from O, S and N, which heterocyclic group may comprise one, two or three rings and which HetA group is optionally substituted by one or more R4b substituents; B represents a Cy2 or HetB; Cy2 represents a 3- to 10-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one or two rings, which Cy2 group is optionally substituted by one or more R4c substituents; HetB represents a 3- to 10-membered heterocyclic group that may be aromatic, fully saturated or partially unsaturated, and which contains one or more heteroatoms selected from O, S and N, which heterocyclic group may comprise one or two rings and which HetB group is optionally substituted by one or more R4d substituents.
Synthesis and anticonvulsant activities of (R)-N-(4′-substituted) benzyl 2-acetamido-3-methoxypropionamides
Salomé, Christophe,Salomé-Grosjean, Elise,Park, Ki Duk,Morieux, Pierre,Swendiman, Robert,DeMarco, Erica,Stables, James P.,Kohn, Harold
supporting information; experimental part, p. 1288 - 1305 (2010/07/10)
The structure-activity relationship (SAR) for the N-benzyl group in the clinical antiepileptic agent (R)-lacosamide [(R)-N-benzyl 2-acetamido-3- methoxypropionamide, (R)-3] has been explored. Forty-three compounds were prepared and then evaluated at the National Institute of Neurological Disorders and Stroke Anticonvulsant Screening Program for seizure protection in the maximal electroshock (MES) and subcutaneous Metrazol models. Comparing activities for two series of substituted aryl regioisomers (2′, 3′, 4′) showed that 4′-modified derivatives had the highest activity. Significantly, structural latitude existed at the 4′-site. The SAR indicated that nonbulky 4′-substituted (R)-3 derivatives exhibited superb activity, independent of their electronic properties. Activities in the MES test of several compounds were comparable with or exceeded that of (R)-3 and surpassed the activities observed for the traditional antiepileptic agents phenytoin, phenobarbital, and valproate. 2009 American Chemical Society.
NOVEL N-BENZYLAMIDE SUBSTITUTED DERIVATIVES OF 2-(ACYLAMIDO)ACETIC ACID AND 2-(ACYLAMIDO)PROPIONIC ACIDS: POTENT NEUROLOGICAL AGENTS
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Page/Page column 59, (2009/12/27)
A first aspect of the invention is a compound (sometimes also referred to herein as an "active agent" or "active compound") of Formula (I) or ( Ia): or a pharmaceutically acceptable salt or prodrug thereof. Compositions thereof and methods of using the same (e.g. for the treatment of a neurological disease) are also described.
Substituted 4-Hydroxypyrimidine-5-Carboxamides
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Page/Page column 51, (2009/10/01)
The present invention relates to substituted 4-hydroxypyrimidine-5-carboxamides useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
Reactivity of the acids of trivalent phosphorus and their derivatives. Part VI. The reaction of the >P-O- anions with benzyl bromides para-substituted in the phenyl ring
Witt, Dariusz,Rachon, Janusz
, p. 169 - 187 (2007/10/03)
The reaction of p-substituted benzyl bromides with the >P-O- ions in THF, alcohols and toluene as the solvents is described. According to the reduction potential of the p-substituted benzyl bromides and the solvent used the formation of the P-C bond, debromination and/or dimerization occur. The principal process is believed to be X-philic substitution, the dimers are formed through a secondary process via SET from the p-substituted benzyl anions into the p-substituted benzyl bromides.