949898-58-2Relevant academic research and scientific papers
Synthesis of functionalized fluoroalkyl pyrimidines and pyrazoles from fluoroalkyl enones
Shaitanova, Elena N.,Balabon, Olga A.,Rybakova, Antonina N.,Khlebnicova, Tatyana S.,Lakhvich, Fedor A.,Gerus, Igor I.
, (2021/11/09)
The synthesis of a series of polyfluoromethyl-substituted pyrimidines and pyrazoles bearing potential for further functionalization of the hydroxymethyl group prepared from the fluoroalkyl-containing enones with isothioureas, amidine and hydrazines, is reported. We investigated the deoxyfluorination of hydroxymethyl group in polyfluoromethyl containing pyrazoles and obtained di- and trifluoromethyl pyrazoles with an additional monofluoromethyl group.
Regioselective Synthesis of Functionalized 3- or 5-Fluoroalkyl Isoxazoles and Pyrazoles from Fluoroalkyl Ynones and Binucleophiles
Chalyk, Bohdan A.,Khutorianskyi, Andrii,Lysenko, Andrii,Fil, Yulia,Kuchkovska, Yuliya O.,Gavrilenko, Konstantin S.,Bakanovych, Iulia,Moroz, Yurii S.,Gorlova, Alina O.,Grygorenko, Oleksandr O.
, p. 15212 - 15225 (2019/11/19)
A facile synthetic route toward either 3- or 5-fluoroalkyl-substituted isoxazoles or pyrazoles containing an additional functionalization site was developed and applied on a multigram scale. The elaborated approach extends the scope of fluoroalkyl substituents for introduction into the heterocyclic moiety, and uses convenient transformations of the side chain for incorporation of fluoroalkyl-substituted azoles into the structures of biologically active molecules. The utility of the obtained building blocks for isosteric replacement of alkyl-substituted isoxazole and pyrazole was shown by the synthesis of fluorinated Isocarboxazid and Mepiprazole analogues.
HETEROARYL COMPOUNDS USEFUL AS INHIBITORS OF SUMO ACTIVATING ENZYME
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Paragraph 00187, (2015/01/16)
Disclosed are compounds of formula (I): or a pharmaceutically acceptable salt thereof; wherein Y, Ra, Ra', Rc, Rf, X2, Rd, Rd', Re, Re', m, and G have the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry, useful as inhibitors of Sumo Activating Enzyme (SAE). Further provided are pharmaceutical compositions comprising a compound of the disclosure and methods of using the compositions in the treatment of proliferative, inflammatory, cardiovascular and neurodegenerative diseases or disorders.
COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY
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Page/Page column 34-35, (2011/04/26)
The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.
Non-nucleoside inhibitors of the measles virus RNA-dependent RNA polymerase complex activity: Synthesis and in vitro evaluation
Sun, Aiming,Chandrakumar, Nizal,Yoon, Jeong-Joong,Plemper, Richard K.,Snyder, James P.
, p. 5199 - 5203 (2008/02/12)
High-throughput screening has identified 1-methyl-3-(trifluoromethyl)-N-[4-(pyrrolidinylsulfonyl)phenyl]-1H-pyrazole-5-carboxamide 16677 as a novel and potent (IC50 = 35-145 nM) inhibitor against multiple primary isolates of diverse measles vir
