25357-43-1Relevant academic research and scientific papers
Novel indolizine derivatives with unprecedented inhibitory activity on human farnesyltransferase
Dumea, Carmen,Belei, Dalila,Ghinet, Alina,Dubois, Jolle,Farce, Amaury,Bcu, Elena
supporting information, p. 5777 - 5781 (2015/01/08)
The rational structural modification of new substituted indolizin-3-yl(phenyl)methanones 1a-i, 2a-i and 3a-i has greatly improved human farnesyltransferase inhibition. The para-bromophenyl analog 2f bearing an ester unit on the indolizine ring demonstrates the highest inhibition potential, with IC50 value of 1.3 ± 0.2 μM. The amidic series 1a-i proves to be the most promising for future modulations, particularly at the triple bond level.
Microwave-assisted, one-pot three component synthesis of 2-phenyl H-imidazo[1, 2-α]pyridine
Motevalli, Kourosh,Yaghoubi, Zahra,Mirzazadeh, Roghieh
experimental part, p. 1047 - 1052 (2012/06/01)
A novel synthesis of 2-phenylH-imidazio[1, 2-α] pyridines is described from a one-pot, three-component reaction between pyridine, guanidine (urea or thiourea) and α-bromoketones under microwave irradiation and solvent-free conditions in excellent yields.
Microwave-assisted, one-pot reaction of pyridines, -bromoketones and ammonium acetate: An efficient and simple synthesis of Imidazo[1,2- a ]-pyridines
Adib, Mehdi,Mohamadi, Ali,Sheikhi, Ehsan,Ansari, Samira,Bijanzadeh, Hamid Reza
experimental part, p. 1606 - 1608 (2010/08/20)
A novel and efficient synthesis of imidazo[1,2-a]pyridines is described. N-Phenacylpyridinium bromides, which were prepared in situ from the addition of pyridines to -bromoketones, undergo nucleophilic addition of ammonium acetate under microwave irradiation and solvent-free conditions to afford the corresponding imidazo[1,2-a]pyridines in excellent yields.
Kinetics and Mechanism of the Pyridinolysis of Phenacyl Bromides in Acetonitrile
Koh, Han Joong,Han, Kwang Lae,Lee, Hai Whang,Lee, Ikchoon
, p. 4706 - 4711 (2007/10/03)
Kinetic studies of the reactions of substituted phenacyl bromides (YC6H4COCH2Br) with pyridines (XC5H4N) are carried out in acetonitrile at 45.0°C. A biphasic Bronsted plot is obtained with a change in slope from a large (βX ? 0.65-0.80) to a small (βX ? 0.36-0.40) value at pKao = 3.2-3.6, which can be attributed to a change in the rate-determining step from breakdown to formation of a tetrahedral intermediate in the reaction path as the basicity of the pyridine nucleophile increases. This mechanism is supported by the faster rates with pyridines than with anilines and the change of cross-interaction constant ρXY from a large positive (ρXY ? +1.4) to a small positive (ρXY ? +0.1) value. The large magnitude of Hammett ρX (= -5.5 to -6.9) values for the pyridines with electron-withdrawing substituents and positive deviations of the π-acceptors, p-CH3CO and p-CN, are quite similar to those for the pyridinium ion formation equilibria. The activation parameters are also in line with the proposed mechanism.
A Synthetic Approach toward the Synthesis of Indolizines via 1,3-Dipolar Cycloaddition Reactions of Cycloimmonium Ylide
Tewari, Ram S.,Bajpai, Anita
, p. 505 - 507 (2007/10/02)
Dehydrohalogenation of N-(2-aroylmethyl)-2-picolinium and -4-picolinium bromide, prepared by the quaternization of corresponding bromide salt with triethylamine, afforded a highly reactive cycloimmonium ylide.Its 1,3-dipolar cycloaddition reactions with v
SYNTHESIS OF FLUORO DERIVATIVES OF 2,4,6-TRIARYLPYRIDINES
Tewari, R. S.,Bajpai, Anita
, p. 319 - 324 (2007/10/02)
A variety of fluoro-substituted 2,4,6-triarylpyridines have been prepared via the reaction of 4-picolinium 4-chlorophenacyl methylide, with a series of fluorinated α,β-unsaturated ketones in the presence of ammonium acetate in acetic acid.
Studies on Cycloimmonium Ylides. Synthesis of Some 2,4,6-Triaryl-Substituted Pyridines via Picolinium Ylides
Tewari, Ram. S.,Dubey, Ajay K.,Misra, Naresh K.,Dixit, Priya D.
, p. 106 - 108 (2007/10/02)
A wide variety of 2,4,6-triaryl-substituted pyridines have been synthesized by the interaction of aroylmethylenepicolinium ylides with different α,β-unsaturated ketones.The structural assignments were based on microanalytical and spectral data.
