6635-61-6Relevant academic research and scientific papers
Room temperature solvent free aza-Michael reactions over nano-cage mesoporous materials
Kalita, Pranjal,Pegu, Choitayna Dev,Dutta, Prantu,Baruah, Pranjal K.
, p. 145 - 150 (2014/08/18)
An efficient highly acidic three dimensional mesoporous aluminosilicate nano-cage material Al-KIT5, exhibited excellent catalytic activity in solvent free room temperature aza-Michael reactions of amines with α,β- unsaturated carbonyl compounds to produce β-amino carbonyl compounds with 100% product selectivity in a short reaction time. The high acidity, 3D pores, and a huge space in the nano-cages materials make them attractive candidate for carrying out important organic reactions. The catalyst provide a simple, easy to handle method, and could be used to solve the problems of corrosion, toxicity, waste production, and a high cost that are being currently encountered by the conventional homogeneous catalysts.
Titania nanoparticles stabilized HPA in SBA-15 for the intermolecular hydroamination of activated olefins
Sawant-Dhuri, Dhanashri,Balasubramanian, Veerappan V.,Ariga, Katsuhiko,Park, Dae-Hwan,Choy, Jin-Ho,Cha, Wang Soo,Al-Deyab, Salem S.,Halligudi, Shivappa B.,Vinu, Ajayan
, p. 3347 - 3354 (2015/04/16)
A liquid phase hydroamination (HA) of α,β-ethylenic compounds with amines was investigated with TiO2 nanoparticles stabilized 12-tungstophosphoric acid (TPA) in SBA-15. The catalysts were prepared by wet impregnation of TPA/TiO2 nanoparticles into the SBA-15 and calcined at different temperatures. The characterization results reveal that the textural properties and the acidity of the prepared catalysts can be finely controlled with the simple adjustment of the calcination temperature and the structure of the support, decorated with the TiO2 and TPA nanoparticles, was intact even after the modification. The prepared catalysts were investigated for HA of ethyl acrylate with different aromatic and aliphatic amines over a wide range of reaction conditions to optimize the yield and the selectivity of product. It was found that this process is 100% atom efficient and the catalytic performance depended significantly on the loading of TPA over the catalyst and the calcination temperature. Under optimized reaction conditions, the best catalyst, 15 wt%TPA/22.4 wt%TiO2/SBA-15 calcined at 1123 K, offered the highest conversion of p-ethylaniline (70%) with 100% chemo-selectivity to the anti-Markovnikov product, i.e., the mono-addition product. The reaction was heterogeneously catalyzed and no contribution from leached TPA into the reaction was observed.
Promiscuous Candida antarctica lipase B-catalyzed synthesis of β-amino esters via aza-Michael addition of amines to acrylates
Dhake, Kishor P.,Tambade, Pawan J.,Singhal, Rekha S.,Bhanage, Bhalchandra M.
experimental part, p. 4455 - 4458 (2010/09/20)
An efficient protocol for the regioselective aza-Michael addition of amines with acrylates using CaL B as a biocatalyst at 60 °C has been developed. The reaction is applicable to a wide variety of primary and secondary amines with different acrylates to synthesize the corresponding β-amino esters with good yields. An alternative route for the synthesis of higher β-amino esters through the additional transesterification step is also studied and was found effective.
Pyrido[2,3-d]pyrimidin-5-ones: A novel class of antiinflammatory macrophage colony-stimulating factor-1 receptor inhibitors
Huang, Hui,Hutta, Daniel A.,Rinker, James M.,Hu, Aping,Parsons, William H.,Schubert, Carsten,Desjarlais, Renee L.,Crysler, Carl S.,Chaikin, Margery A.,Donatelli, Robert R.,Chen, Yanmin,Cheng, Deping,Zhou, Zhao,Yurkow, Edward,Manthey, Carl L.,Player, Mark R.
experimental part, p. 1081 - 1099 (2010/01/07)
A series of pyrido[2,3-d]pyrimidin-5-ones has been synthesized and evaluated as inhibitors of the kinase domain of macrophage colony-stimulating factor-1 receptor (FMS). FMS inhibitors may be useful in treating rheumatoid arthritis and other chronic infla
POLO-LIKE KINASE INHIBITORS
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Page/Page column 169, (2009/06/27)
Compounds of the following formula are provided for use with kinases, wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful
5-OXO-5,8-DIHYDRO-PYRIDO-PYRIMIDINES AS INHIBITORS OF C-FMS KINASE
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Page/Page column 84, (2008/12/05)
The invention addresses the current need for selective and potent protein tyrosine kinase inhibitors by providing potent inhibitors of c-fms kinase. The invention is directed to the novel compounds of Formula I: or a salt, stereoisomer, tautomer, crystalline, polymorph, amorphous, solvate, hydrate, ester, prodrug or metabolite form thereof, wherein A, Y, Z, R101 and R200 are described in the specification.
Design and synthesis of a pyrido[2,3-d]pyrimidin-5-one class of anti-inflammatory FMS inhibitors
Huang, Hui,Hutta, Daniel A.,Hu, Huaping,DesJarlais, Renee L.,Schubert, Carsten,Petrounia, Ioanna P.,Chaikin, Margery A.,Manthey, Carl L.,Player, Mark R.
, p. 2355 - 2361 (2008/09/20)
A series of pyrimidinopyridones has been designed, synthesized and shown to be potent and selective inhibitors of the FMS tyrosine kinase. Introduction of an amide substituent at the 6-position of the pyridone core resulted in a significant potency increase. Compound 24 effectively inhibited in vivo LPS-induced TNF in mice greater than 80%.
PARAKERATOSIS INHIBITOR, PORE-SHRINKING AGENT AND EXTERNAL COMPOSITION FOR SKIN
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Page/Page column 23, (2008/06/13)
The invention provides a parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/amaliorating agent that has a function such as parakeratosis inhibition, pore shrinkage, or rough skin -inhibition/abatement, poses no safety problems such as sensory irritation, and is very safe, and further provides an external composition for skin to which a compound having the above-mentioned function has been added. The parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/amaliorating agent comprises one or more compounds selected from the group consisting of β-alanine derivatives and salts thereof. The external composition for skin comprises the one or more compounds selected from the group consisting of β-alanine derivatives and salts thereof as the above-mentioned parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/amaliorating agent.
WRINKLE-IMPROVING AGENT
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Page/Page column 20-21, (2008/12/06)
The invention provides a novel wrinkle-improving agent that has an effect of improving wrinkles, that does not entail problems of safety or pain even when applied to the skin, and that contains a very safe substance as an active component. A discovery was made that N-benzoyl-β-alanine, other specific β-alanine derivatives, and salts thereof have a wrinkle-improving effect, whereby a wrinkle-improving agent containing as an active component one, two, or more types of compounds selected from the group composed of these specific β-alanine derivatives and the salts thereof was developed.
5-Oxo-5,8-dihydro-pyrido-pyrimidines as inhibitors of c-fms kinase
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Page/Page column 34, (2008/06/13)
The invention addresses the current need for selective and potent protein tyrosine kinase inhibitors by providing potent inhibitors of c-fms kinase. The invention is directed to the novel compounds of Formula I: or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof, wherein:W, A, Y, n, Z, and R102 are described in the specification.
