- Ethylene diamine grafted nanoporous UiO-66 as an efficient basic catalyst in the multi-component synthesis of 2-aminithiophenes
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This study demonstrates ED-UiO-66 as a novel and effective solid nanoporous basic catalyst prepared through the amine grafting onto the pores of UiO-66. The manufactured nanoparticles were identified by FT-IR, XRD, TGA, FESEM, TEM, CHN and BET and the characterization results certified formation of a single phase nanoporous substance with the medium grain size less than 90?nm. The synthesized material was employed as an efficient catalyst for the preparation of 2-aminotiophenes through the Gewald method. This thermochemically stable nanocatalyst was environmentally safe, reusable and economic. Therefore, this methodology can be simply extended for industrial goals.
- Erfaninia,Tayebee,Dusek,Amini
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- Synthesis and evaluation of 4-anilinoquinazoline bioisosteres as potential anti-breast cancer agents
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Based on one of the four major categories of scaffold hopping theory namely hetrocycle replacements, a series of 5-arylthieno[2,3-d]pyrimidines had been prepared and evaluated as anti-breast cancer agents. Optimization by combination of different pharmacophores with the thienopyrimidine scaffold led to discovery of biologically active compounds.
- El-Ansary, Afaf K.,Kamal, Aliaa M.,Al-Ghorafi, Mokhtar Abdhafiz
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p. 202 - 210
(2014/09/29)
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- Easy single-step preparation of ZnO nano-particles by sedimentation method and studying their catalytic performance in the synthesis of 2-aminothiophenes via Gewald reaction
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Zinc oxide is a multi-purpose active material with important catalytic applications. In this study, nano-sized ZnO particles were easily synthesized through sedimentation of zinc acetate di-hydrate in absolute ethanol and were characterized by XRD and SEM. The XRD results indicated pure wurtzite structure with the average particle size of 26.9 nm for the nano-particles. It was observed that size of ZnO nano-particles was decreased while solution concentration was increased. This observation would be explained considering enhancing nucleation processes of nano-particles at high concentration of zinc acetate. The prepared nano-particles (2.5 mol%) were used as catalyst for the fast and efficient synthesis of 2-aminothiophenes under solvent free conditions. The three-component mixture of a carbonyl compound, malonodinitrile, and elemental sulfur was converted into the corresponding 2-aminothiophene in moderate to high yields with excellent selectivity.
- Tayebee, Reza,Javadi, Farzad,Argi, Gholamreza
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- Crystalline N-(4-(4-aminothieno[2,3-d]pyrimidin-5-yl)phenyl)-N'-(2-fluoro-5-(trifluoromethyl)phenyl)urea ethanolate
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A crystalline N-(4-(4-aminothieno[2,3-d]pyrimidin-5-yl)phenyl)-N′-[2-fluoro-5-(trifluoromethyl)phenyl)urea ethanolate, ways to make it, compositions comprising it, and methods of treatment using it are disclosed.
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Page/Page column 3
(2008/06/13)
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- Crystalline N-(4-(4-ammoniumthieno[2,3-d]pyrimidin-5-yl)phenyl)-N'-(2-fluoro-5-(trifluoromethyl)phenyl)urea ethanesulfonate
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A crystalline N-(4-(4-ammoniumthieno[2,3-d]pyrimidin-5-yl)phenyl)-N′-(2-fluoro-5-(trifluoromethyl)phenyl)urea ethanesulfonate, ways to make it, compositions comprising it, and methods of treatment using it are disclosed.
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Page/Page column 3
(2008/06/13)
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- A practical and selective reduction of nitroarenes using elemental sulfur and mild base
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A method was developed to reduce aromatic nitro compounds to the corresponding anilines using sulfur and base. The method tolerates a range of functional groups on the benzene ring, avoids the use of hydrogen and transition metals and provides the anilines in moderate to high yields.
- McLaughlin, Maureen A.,Barnes, David M.
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p. 9095 - 9097
(2007/10/03)
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- New conditions for the synthesis of thiophenes via the Knoevenagel/Gewald reaction sequence. Application to the synthesis of a multitargeted kinase inhibitor
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Novel conditions have been developed for the preparation of substituted 2-aminothiophenes employing the Knoevenagel condensation followed by the Gewald reaction. The benefits of these conditions are their mildness, and the ease of product isolation. Thus,
- Barnes, David M.,Haight, Anthony R.,Hameury, Thomas,McLaughlin, Maureen A.,Mei, Jianzhang,Tedrow, Jason S.,Riva Toma, Joan Dalla
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p. 11311 - 11319
(2007/10/03)
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- Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors
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A series of novel thienopyrimidine-based receptor tyrosine kinase inhibitors has been discovered. Investigation of structure-activity relationships at the 5- and 6-positions of the thienopyrimidine nucleus led to a series of N,N′-diaryl ureas that potentl
- Dai, Yujia,Guo, Yan,Frey, Robin R.,Ji, Zhiqin,Curtin, Michael L.,Ahmed, Asma A.,Albert, Daniel H.,Arnold, Lee,Arries, Shannon S.,Barlozzari, Teresa,Bauch, Joy L.,Bouska, Jennifer J.,Bousquet, Peter F.,Cunha, George A.,Glaser, Keith B.,Guo, Jun,Li, Junling,Marcotte, Patrick A.,Marsh, Kennan C.,Moskey, Maria D.,Pease, Lori J.,Stewart, Kent D.,Stoll, Vincent S.,Tapang, Paul,Wishart, Neil,Davidsen, Steven K.,Michaelides, Michael R.
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p. 6066 - 6083
(2007/10/03)
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- Thiopyrimidine and isothiazolopyrimidine kinase inhibitors
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Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
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Page/Page column 21
(2008/06/13)
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- Thiopyrimidine and isothiazolopyrimidine kinase inhibitors
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Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compound, compositions containing the compounds, and methods of treatment using the compounds.
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- Thiopyrimidine and isothiazolopyrimidine kinase inhibitors
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Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
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