210992-56-6Relevant articles and documents
Practical and economic lithiations of functionalized arenes and heteroarenes using Cy2NLi in the presence of Mg, Zn or La halides in a continuous flow
Becker, Matthias R.,Ganiek, Maximilian A.,Knochel, Paul
, p. 6649 - 6653 (2015/10/28)
The economic amide base lithium dicyclohexylamide (Cy2NLi) allows fast and convenient (40 s, 0°C) in situ trapping flow metalations of a broad range of functionalized arenes, heteroarenes and acrylate derivatives in the presence of various meta
One-pot double functionalisation of π-deficient heterocyclic lithium reagents
Chartoire, Anthony,Comoy, Corinne,Fort, Yves
experimental part, p. 1839 - 1845 (2011/04/26)
Herein, we report an efficient method for the double functionalisation of lithiated halogenopyridines, -pyrazines or -furopyridines through a convenient one-pot electrophilic trapping/nucleophilic substitution sequence.
Intrinsic electrophilicity of the 4-methylsulfonyl-2-pyridone scaffold in glucokinase activators: Role of glutathione-S-transferases and in vivo quantitation of a glutathione conjugate in rats
Litchfield, John,Sharma, Raman,Atkinson, Karen,Filipski, Kevin J.,Wright, Stephen W.,Pfefferkorn, Jeffrey A.,Tan, Beijing,Kosa, Rachel E.,Stevens, Benjamin,Tu, Meihua,Kalgutkar, Amit S.
scheme or table, p. 6262 - 6267 (2010/11/18)
Previous studies on the in vitro metabolism of 4-alkylsulfonyl-2-pyridone- based glucokinase activators revealed a facile, non-enzymatic displacement of the 4-alkylsulfonyl group by glutathione. In the present studies, a role for glutathione-S-transferases (GST) as catalysts in the desulfonylation reaction was demonstrated using a combination of human liver microsomes, human liver cytosol and human GSTs. The identification of a glutathione conjugate in circulation following intravenous administration of a candidate 4-methylsulfonyl-2-pyridone to rats confirmed the relevance of the in vitro findings.
Pyrazole derivatives
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, (2019/07/22)
The present invention relates to cis- and trans-forms of pyrazole derivatives, salts thereof, or agents containing the same, and represented by the general formula (I): wherein G represents a nitrogen containing saturated heterocyclic structure represented by the following formula: These compounds exhibit anti-tumor activity on 5-FU-resistant tumors and effects on P glycoprotein expressing, multiple-drug resistant tumors. An example of a pyrazole derivative which demonstrates 50% inhibition of tumor cell growth is 3-[4-(3-chloro-5-fluorophenyl)-1 piperazinyl]-1-[1-(3-chloro-2-pyridyl)-5-methyl-4-pyrazolyl)-1-trans-propene hydrochloride. Synthesis of the compounds represented by formula (I) can be prepared by any one of various routes such as a Mannich reaction, a Wittig reaction, reductive amination or substitution by allylation.
