1291099-87-0Relevant academic research and scientific papers
Alternative approaches to the synthesis of polyfluoroalkyl-containing 1-methyl-4-nitrosopyrazoles
Agafonova, N. A.,Burgart, Ya. V.,Evstigneeva, N. P.,Gerasimova, N. A.,Saloutin, V. I.
, p. 1135 - 1140 (2021)
We studied different approaches to the synthesis of polyfluoroalkyl-containing 1-methyl-4-nitrosopyrazoles, which are based on the cyclization of 4,4,4-trifluoro-3,3-dihydroxy-2-hydroxyimino-1-R-butan-1-ones or 2-hydroxyimino-1,3-diketones with methylhydrazine and on a one-pot sequential treatment of 1,3-diketones with sodium nitrite and methylhydrazine. It was found that the regioselectivity of the formation of 1-methyl-4-nitrosopyrazoles is affected by the steric factors of 1,3-dicarbonyl reagents. The study of the mycostatic effect of 4-nitrosopyrazoles showed that the introduction of a bulky polyfluoroalkyl or tert-butyl substituent leads to a decrease in their activity.
Multiple biological active 4-aminopyrazoles containing trifluoromethyl and their 4-nitroso-precursors: Synthesis and evaluation
Agafonova, Natalia A.,Borisevich, Sophia S.,Burgart, Yanina V.,Chupakhin, Oleg N.,Evstigneeva, Natalia P.,Gerasimova, Natalia A.,Krasnykh, Olga P.,Kungurov, Nikolai V.,Kushch, Svetlana O.,Makhaeva, Galina F.,Maslova, Vera V.,Rudakova, Elena V.,Saloutin, Victor I.,Shchegolkov, Evgeny V.,Solodnikov, Sergey Yu.,Triandafilova, Galina A.,Ulitko, Maria V.,Zilberberg, Natalia V.
, (2020/09/16)
4-Nitroso-3-trifluoromethyl-5-alkyl[(het)aryl]pyrazoles were synthesized via one-pot nitrosation of 1,3-diketones or their lithium salts followed by treatment of hydrazines. Reduction of nitroso-derivatives made it possible to obtain 4-amino-3-trifluorome
THIAZOLYL AND OXAZOLYL UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS AS TRKA KINASE INHIBITORS
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, (2014/06/11)
Compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.
BICYCLIC HETEROARYL UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS AS TRKA KINASE INHIBITORS
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, (2014/06/11)
Compounds of Formula I or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis and pelvic pain syndrome.
BICYCLIC UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS USEFUL FOR THE TREATMENT OF PAIN
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, (2014/06/11)
Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis and pelvic pain syndrome.
One-pot synthesis of trifluoromethyl-and nitroso-substituted pyrazolines and pyrazoles and their tuberculostatic activity
Khudina,Burgart,Saloutin,Kravchenko
experimental part, p. 1967 - 1973 (2011/06/27)
3-Trifluoromethyl-substituted 4-nitrosopyrazolines and 4-nitrosopyrazoles were prepared by a one-pot synthesis from trifluoromethyl-containing 1,3-diketones, sodium nitrite in acetic acid, and hydrazines (hydrazine hydrate, methylhydrazine). 3-Trifluorome
