69422-57-7Relevant academic research and scientific papers
BRD4-JAK2 INHIBITORS
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Page/Page column 39, (2020/03/29)
Disclosed herein are compounds that are inhibitors of BDR4 and their use in the treatment of cancer. Methods of screening for selective inhibitors of BDR4 are also disclosed. In certain aspects, disclosed are compounds of Formula I, II, and II.
Synthesis of N-carboxyalkyl-1,4-benzothiazepine-3(2H)-one derivatives using esters of N-(2-chloro-5-nitrobenzyl)amino acids
Tarasiuk, Taras M.,Volovnenko, Tetiana A.,Volovenko, Yulian M.,Medviediev, Volodymyr V.,Shishkin, Oleg V.
, p. 483 - 489 (2014/03/21)
Two alternative approaches for synthesis of esters of N-(2-chloro-5- nitrobenzyl) amino acids have been developed and compared. We have found synthesis of N-(2-chloro-5-nitrobenzyl) amino acids via alkylation of esters of amino acids in DMF in the presence of Et3N and NaI to be more convenient and have higher yields in comparison with reduction of Schiff bases obtained from 2-chloro-5-nitrobenzaldehyde and corresponding esters of amino acids by NaBH4. Treatment of the solutions of esters of N-(2-chloro-5-nitrobenzyl) amino acids in DMSO with methyl thioglycolate and following intramolecular acylation in xylene led to N-carboxyalkyl-1,4- benzothiazepine-3(2H)-one derivatives in 24-76 % yields. Graphical abstract: [Figure not available: see fulltext.]
METHODS OF SYNTHESIZING 2-METHOXYMETHYL-1,4-BENZENEDIAMINE
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Page/Page column 6-7, (2012/04/17)
Disclosed is a method of making 2-methoxymethyl-1,4-benzenediamine that includes hydrogenating 1-benzylamino-2-(methoxymethyl)-4-nitrobenzene in the presence of a hydrogenation catalyst.
A substrate-driven approach to determine reactivities of α,β-unsaturated carboxylic esters towards asymmetric bioreduction
Tasnádi, Gábor,Winkler, Christoph K.,Clay, Dorina,Sultana, Nargis,Fabian, Walter M. F.,Hall, Mélanie,Ditrich, Klaus,Faber, Kurt
supporting information; experimental part, p. 10362 - 10367 (2012/10/08)
The degree of C=C bond activation in the asymmetric bioreduction of α,β-unsaturated carboxylic esters by ene-reductases was studied, and general recommendations to render these "borderline-substrates" more reactive towards enzymatic reduction are proposed. The concept of "supported substrate activation" was developed. In general, an additional α-halogenated substituent proved to be beneficial for enzymatic activity, whereas β-alkyl or β-aryl substituents were detrimental for the reactivity of nonhalogenated substrates, and α-cyano groups showed little effect. The alcohol moiety of the ester functionality was found to have a strong influence on the reaction rate. Overall, activities were determined by both steric and electronic effects. Biotransformation: The asymmetric bioreduction of α,β-unsaturated carboxylic esters by ene-reductases could be tuned by varying the degree of C=C bond activation (see scheme). An additional α-halogenated substituent proved to be beneficial for enzymatic activity, whereas β-alkyl or β-aryl substituents were detrimental for the reactivity of nonhalogenated substrates. Copyright
Methods of Synthesizing 2-Substituted-1,4-Benzenediamine
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Page/Page column 7, (2012/04/05)
Disclosed is a method of making a 2-substituted-1,4-benzenediamine by nucleophilic aromatic substitution.
Synthesis and herbicidal activity of 1,5-diarylpyrazole derivatives
Kudo, Noriaki,Furuta, Satoru,Taniguchi, Misa,Endo, Takeshi,Sato, Kazuo
, p. 857 - 868 (2007/10/03)
A series of diarylpyrazolecarboxylates and carboxamides were prepared, and their herbicidal activities were investigated. Some of these compounds showed noticeable pre-emergent herbicidal activities against various kinds of weeds. Among the synthesized co
