89607-12-5Relevant academic research and scientific papers
Compound with BRD4 inhibitory activity, preparation method and application thereof
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Paragraph 0838-0843; 1007-1011, (2021/04/10)
The invention discloses a compound with BRD4 inhibitory activity, a preparation method and application thereof. The structure of the compound with the BRD4 inhibitory activity is shown as a formula I, and definitions of substituent groups are shown in the specification and claims. The compound provided by the invention has very high bromodomain protein inhibition activity, especially BRD4 targeted inhibition activity, and can be used for treating or/and preventing related diseases mediated by bromodomain protein.
Cyclic Meso-ionic Compounds. Part 21. The Examination of Nitro-derivatives of Meso-ionic Heterocycles as Potential Pharmaceuticals
Newton, Christopher G.,Ollis, W. David,Podmore, Michael L.,Wright, Derek E.
, p. 63 - 67 (2007/10/02)
The synthesis of nitro-substituted meso-ionic compounds has been examined in an attempt to obtain analogues of the biologically active heterocycles (1)-(3).The synthesis of the compounds (4) and (5) has been achieved but their instability precluded biological evaluation.The synthesis of the type-B meso-ionic heterocycle (6) was not successfully completed, but unusual nucleophilic displacement reactions of the pyrazole (13) -> (16) + (17) and the pyrazolium salt (14) -> (15) are reported.
SYNTHESIS OF 3-AMINO-4-NITROPYRAZOLES
Perevalov, V. P.,Andreeva, M. A.,Baryshnenkova, L. I.,Manaev, Yu. A.,Yamburg, G. S.,et al.
, p. 1326 - 1330 (2007/10/02)
3-Bromo-1,5-dimethyl-4-nitropyrazole does not react upon heating with aqueous ammonia, while 1,5-dimethyl-3,4-dinitropyrazole under the same conditions yields 3-amino-1,5-dimethyl-4-nitropyrazole, which is formed from 3-bromo-1,5-dimethyl-4-nitropyrazole in the presence of a copper catalyst.The amination of 1-methyl-3,4-dinitropyrazole-5-carboxylic acid is accompanied by decarboxylation, which is characteristic for 4-substituted 1-methylpyrazole-5-carboxylic acids upon heating in aqueous ammonia or water.
AMINATION OF ISOMERIC BROMO-1-METHYLNITROPYRAZOLES
Perevalov, V. P.,Baryshnenkova, L. I.,Andreeva, M. A.,Manaev, Yu. A.,Denisova, I. A.,et al.
, p. 1322 - 1326 (2007/10/02)
A method was developed for the synthesis of 5-bromo-1-methyl-4-nitropyrazole from 1-methylpyrazole.In the reaction with 25percent aqueous ammonia at 180-190 deg C, 5-bromo-1-methyl-4-nitropyrazole is readily converted to 5-amino-1-methyl-4-nitropyrazole; the production of 4-amino-1-methyl-5-nitropyrazole from 4-bromo-1-methyl-5-nitropyrazole requires the presence of a copper catalyst; under the same conditions in the amination of 4-bromo-1-methyl-3-nitropyrazole, 4-amino-1-methyl-3-nitro- and 1-methyl-3-nitropyrazoles are formed in a 2 : 3 ratio.
