- Mild Darzens Annulations for the Assembly of Trifluoromethylthiolated (SCF3) Aziridine and Cyclopropane Structures
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We report mild new annulation approaches to trisubstituted trifluoromethylthiolated (SCF3) aziridines and cyclopropanes via Darzens inspired protocols. The products of these anionic annulations, rarely studied previously, possess attractive features rendering them valuable building blocks for synthesis platforms. In this study, trisubstituted acetophenone nucleophiles bearing SCF3 and bromine substituents in their α position were shown to undergo [2 + 1] annulations with vinyl ketones and tosyl-protected imines under mild reaction conditions.
- Delost, Michael D.,Njardarson, Jon T.
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supporting information
p. 6121 - 6125
(2021/08/16)
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- Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase Inhibitors
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Janus kinases (JAKs) have been demonstrated to be critical in cytokine signaling and have thus been implicated in both cancer and inflammatory diseases. The JAK family consists of four highly homologous members: JAK1-3 and TYK2. The development of small-m
- Grimster, Neil P.,Anderson, Erica,Alimzhanov, Marat,Bebernitz, Geraldine,Bell, Kirsten,Chuaqui, Claudio,Deegan, Tracy,Ferguson, Andrew D.,Gero, Thomas,Harsch, Andreas,Huszar, Dennis,Kawatkar, Aarti,Kettle, Jason G.,Lyne, Paul,Read, Jon A.,Rivard Costa, Caroline,Ruston, Linette,Schroeder, Patricia,Shi, Jie,Su, Qibin,Throner, Scott,Toader, Dorin,Vasbinder, Melissa,Woessner, Richard,Wang, Haixia,Wu, Allan,Ye, Minwei,Zheng, Weijia,Zinda, Michael
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supporting information
p. 5235 - 5244
(2018/06/11)
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- Synthesis and biological evaluation of GPR40/FFAR1 agonists containing 3,5-dimethylisoxazole
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GPR40 is an attractive target due to its glucose-stimulated insulin secretion effect with low risk of causing hypoglycemia, which also can be seen from the clinical studies using TAK-875 (fasiglifam). In the present studies, we discovered a series of anal
- Yang, Lingyun,Zhang, Jian,Si, Lianghui,Han, Li,Zhang, Bo,Ma, Hui,Xing, Junhao,Zhao, Leilei,Zhou, Jinpei,Zhang, Huibin
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- Novel metal oxide nanocomposite of Au/CuO-ZnO for recyclable catalytic aerobic oxidation of alcohols in water
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CuO-ZnO supported gold nanoparticle is introduced as a new, efficient, and recyclable catalyst for the aerobic oxidation of alcohols. The CuO-ZnO support was prepared by co-precipitation and Au nanoparticles were loaded on support by a deposition-precipitation method. The catalyst was characterized by XRD, BET surface area, FESEM, EDS and HRTEM techniques. A wide range of alcohols, including benzylic, primary and secondary alcohols are converted into the corresponding carbonyl derivatives. The experimental procedure with Au/CuO-ZnO catalyst is quite straightforward and the catalyst is recyclable up to 6 consecutive runs by simple filtration.
- Albadi, Jalal,Alihoseinzadeh, Amir,Razeghi, Abdolhosein
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- 2 -ARYLAMINOQUINAZOLINES FOR TREATING PROLIFERATIVE DISEASES
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The invention provides novel compounds that are inhibitors of PDKI. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or composition.
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Page/Page column 185
(2010/01/12)
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- Bromination of deactivated aromatics: A simple and efficient method
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(Chemical Equation Presented) Highly deactivated aromatic compounds were smoothly monobrominated by treatment with N-bromosuccinimide (NBS) in concentrated H2SO4 medium affording the corresponding bromo derivatives in good yields. Mild reaction conditions and simple workup provides a practical and commercially viable route for the synthesis of bromo compounds of deactivated aromatics.
- Rajesh,Somasundaram,Saiganesh,Balasubramanian
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p. 5867 - 5869
(2008/02/09)
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- Covalent assembly of molecular ladders
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[n]-Rung molecular ladders (n = 3-6) have been prepared by reacting discrete, complimentary m-phenylene ethynylene oligomers using imine formation/exchange. The nanostructures, which in the largest case measure approximately 1.6 × 6.2 nm, have been charac
- Hartley, C. Scott,Elliott, Erin L.,Moore, Jeffrey S.
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p. 4512 - 4513
(2007/10/03)
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