52096-24-9Relevant articles and documents
Protonated alkylpyrazole ionic liquid and method using same for synthesizing cyclic carbonate
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Paragraph 0026; 0028, (2018/01/12)
The invention relates to protonated alkylpyrazole ionic liquid with a structural formula as shown in the description, wherein n is equal to 1, 2, 3 or 4, and X is Cl, Br or I. The invention further discloses a method for synthesizing cyclic carbonate by using the protonated alkylpyrazole ionic liquid; the protonated alkylpyrazole ionic liquid and an epoxy compound are added into a high-pressure reaction kettle according to a molar ratio of 1 : (25 to 300), CO2 is introduced until pressure is 1-3 MPa, and constant-temperature constant-pressure reaction is performed for 1-5 hours at a temperature of 100-150 DEG C, and post-treatment is performed after reaction is ended, thus obtaining the cyclic carbonate. The method solves the problems that CO2 activation is difficulty, a catalyst is dear, a poisonous organic solvent is used, a synthesis process is complex, reaction conditions are harsh and the like in an existing method. The advantages of simple synthesis process, high catalyst activity, environmental friendliness, low cost and the like are achieved.
Sonochemical heating profile for solvents and ionic liquid doped solvents, and their application in the N-alkylation of pyrazoles
Frizzo, Clarissa P.,Bacim, Carolini,Moreira, Dayse N.,Rodrigues, Leticia V.,Zimmer, Geórgia C.,Bonacorso, Hélio G.,Zanatta, Nilo,Martins, Marcos A.P.
, p. 432 - 439 (2016/05/09)
The heating profile for 25 solvents was determined in ultrasonic probe equipment at amplitudes of 20%, 25%, and 30%. Each solvent was heated in accordance with its boiling point. The effect of vapor pressure, surface tension, and viscosity of the solvents in dissipated ultrasonic power (Up) was evaluated. Multiple regression analysis of these solvent properties and dissipated Up reveals that solvent viscosity is the property that most strongly affected dissipated Up. Experimentation involving acetonitrile doped with [BMIM][BF4] indicated faster heating than MeCN. Aprotic polar solvents such as DMSO, DMF, and MeCN were tested in the N-alkylation of pyrazoles under ultrasonic conditions. After 5 min at 90 °C, the reactants had been totally converted into product in these solvents. Solvents, with low dissipated Up (e.g., toluene) were tested. Conversions were lower compared to those of aprotic polar solvents. When the reactions were done in hexane, no conversion to product was observed. To check the effect of doping in solvents with low Up, [BMIM][BF4], DMSO, and DMF were selected. The conversions for toluene doped with [BMIM][BF4], DMSO, and DMF were 100%, 59%, and 25%, respectively. These conversions were greater than when done in just toluene (46%). Thus, [BMIM][BF4] was the best polar doping solvent, followed by DMSO. DMF was not considered to be a satisfactory doping solvent. No conversion was observed for reactions in the absence of base performed in DMSO, DMF, and MeCN doped with [BMIM][BF4].
SMALL MOLECULE INHIBITORS OF IL-6 AND USES THEREOF
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Paragraph 00932, (2013/03/26)
In one aspect, the invention relates to substituted 2-(lH-indol-3-yl)ethanol analogs and substituted 3,3a,8,8a-tetrahydro-2H-furo[2,3-b]indole analogs, derivatives thereof, and related compounds, which are useful as inhibitors of IL-6 mediated activation of the Jak2/STAT3 pathway; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a IL6 dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Synthesis and structure-activity relationship of a novel series of heterocyclic sulfonamide γ-secretase inhibitors
Pu, Jun,Kreft, Anthony F.,Aschmies, Suzan H.,Atchison, Kevin P.,Berkowitz, Joshua,Caggiano, Thomas J.,Chlenov, Micheal,Diamantidis, George,Harrison, Boyd L.,Hu, Yun,Huryn, Donna,Steven Jacobsen,Jin, Mei,Lipinski, Kerri,Lu, Peimin,Martone, Robert L.,Morris, Koi,Sonnenberg-Reines, June,Riddell, Dave R.,Sabalski, Joan,Sun, Shaiu-Ching,Wagner, Erik,Wang, Yiqun,Xu, Zheng,Zhou, Hua,Resnick, Lynn
body text, p. 4708 - 4717 (2009/10/23)
γ-Secretase inhibitors have been shown to reduce the production of β-amyloid, a component of the plaques that are found in brains of patients with Alzheimer's disease. A novel series of heterocyclic sulfonamide γ-secretase inhibitors that reduce β-amyloid levels in cells is reported. Several examples of compounds within this series demonstrate a higher propensity to inhibit the processing of amyloid precursor protein compared to Notch, an alternative γ-secretase substrate.
4-AMINO-5-METHYLPYRAZOLE DERIVATIVES AND PROCESS FOR PRODUCTION THEREOF
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Page/Page column 32, (2010/02/14)
The present invention relates to 4-amino-5-methylpyrazole derivatives represented by the following formula (I): (wherein R1 represents an isobutyl group, a cyclobutylmethyl group, a neopentyl group or the like) or a salt thereof, which are novel compounds being useful as synthetic intermediates of pharmaceuticals, agricultural chemicals or the like.
Quaternization and dequaternization of pyrazoles in solvent- free conditions: Conventional heating versus microwave irradiation
Diez-Barra, Enrique,De La Hoz, Antonio,Sanchez-Migallon, Ana,Elguero, Jose
, p. 889 - 894 (2007/10/03)
We report a study on the quaternization and dequaternization of pyrazoles by conventional heating and microwave irradiation in solvent-free conditions. Microwave irradiation produces an acceleration in the quaternization rate and a rapid equilibration between quaternized and non quaternized products. Dequaternization is also more rapid and a change on the selectivity is observed using symmetric pyrazolium salts.
Synthesis of N-Alkylpyrazoles by Phase Transfer Catalysis without Solvent
Diez-Barra, E.,Hoz, A. de la,Sanchez-Migallon, A.,Tejeda, J.
, p. 2849 - 2853 (2007/10/02)
The alkylation of pyrazole is performed by phase transfer catalysis without solvent.High yields of N-alkylpyrazoles are obtained and the principal problems in the alkylation are suitably solved.
Influence of N-substitution in the FVT of pyrazoles
Perez, Jorge D.,Yranzo, Gloria I.,Phagouape, Leonardo M.
, p. 129 - 132 (2007/10/02)
Flash vacuum thermolysis of 1-ethyl (3), 3,5-dimethyl-1-ethyl (4), 1-n-buthyl (5), 1-tert-butyl (6), 3,5-dimethyl-1-phenyl (7) and 1-phenyl-pyrazole (8) was studied.In the N-alkyl derivatives, pyrazole elimination and olefin formation was found.In contrast, phenylderivatives afforded isomerization and nitrogen extrusion.Kinetic parameters for compound 4 are described and a general mechanism including the N-H derivatives is discussed.
ETUDE DANS LA SERIE DES ORGANOSILYLAZOLES I. ACTION DES HALOGENURES D'ALKYLE, DES CHLORURES D'ACIDE ET DES CETONES HALOGENEES
Gasparini, J. P.,Gassend, R.,Maire, J. C.,Elguero, J.
, p. 141 - 150 (2007/10/02)
The reactivity of organosilylamines of imidazole, pyrazole, 1,2,4-triazole and benzotriazole towards alkyl halides, acidic chlorides and halogenated ketones has been studied.Except for 1-trimethylsilylimidazole, which gives a mixed quaternary salt, reactions with primary halides lead to the corresponding 1-alkylated heterocyclic compounds in high yields; in each case only one isomer is obtained (1-alkyl-1,2,4-triazole and 1-alkylbenzotriazole).Similarly acidic chlorides give 1-acylated derivatives in quantitative yields.Finally α- or β-halogenated ketones show different behaviour and give the addition or substitution products.
