58278-92-5Relevant academic research and scientific papers
I2-Promoted [3+2] Cyclization of 1,3-Diketones with Potassium Thiocyanate: a Route to Thiazol-2(3H)-One Derivatives
An, Zhenyu,Liu, Yafeng,Yan, Rulong,Zhao, Pengbo
supporting information, p. 3240 - 3244 (2021/06/16)
An I2-promoted strategy has been developed for the synthesis of thiazol-2(3H)-one derivatives from 1,3-diketones with potassium thiocyanate. This [3+2] cyclization reaction involves C?S and C?N bond formation and exhibits good functional group tolerance. A series of thiazol-2(3H)-one derivatives are obtained in moderate to good yields. (Figure presented.).
Discovery of pyrazole N-aryl sulfonate: A novel and highly potent cyclooxygenase-2 (COX-2) selective inhibitors
Guo, Quanping,Wang, Mengran,Wang, Rui,Xu, Zhaoqing,Yao, Haiyan
, (2021/08/25)
Based on a new pyrazole sulfonate synthetic method, a novel class of molecules with a basic structure of pyrazole N-aryl sulfonate have been designed and synthesized. The interest in conducting intensive research stems from quite evident anti-inflammatory effects exhibited by the compounds in preliminary animal experiments. A series of compounds were synthesized by different substitutions of the R1, R2, and R3 groups. Within the series, 4-iodophenyl 5-methyl-3-(p-tolyl)-1H-pyrazole-1-sulfonate and phenyl 5-methyl-3-(4-(trifluoromethyl) phenyl)-1H-pyrazole-1-sulfonate exhibited excellent anti-inflammatory activity (% inhibition of auricular edemas = 27.0 and 35.9, respectively); the in vivo analgesic activity of phenyl 5-methyl-3-(p-tolyl)-1H-pyrazole-1-sulfonate and 2-chlorophenyl 5-methyl-3-(p-tolyl)-1H-pyrazole-1-sulfonate was confirmed to be effective (inhibition ratio of writhing = 50.7% and 48.5% separately), and compounds phenyl 5-methyl-3-(p-tolyl)-1H-pyrazole-1-sulfonate, 4-iodophenyl 5-methyl-3-(p-tolyl)-1H-pyrazole-1-sulfonate and 2-chlorophenyl 5-methyl-3-(p-tolyl)-1H-pyrazole-1-sulfonate were identified as selective COX-2 inhibitors (SI = 455, 10,497 and >189 severally). In Acute Oral Toxicity assays conducted in vivo, the lethal dose 50 (LD50) of 4-iodophenyl 5-methyl-3-(p-tolyl)-1H-pyrazole-1-sulfonate and 2-chlorophenyl 5-methyl-3-(p-tolyl)-1H-pyrazole-1-sulfonate to mice was >2000 mg/kg BW.
COtab: Expedient and Safe Setup for Pd-Catalyzed Carbonylation Chemistry
Collin, Hugo P.,Reis, Wallace J.,Nielsen, Dennis U.,Lindhardt, Anders T.,Valle, Marcelo S.,Freitas, Rossimiriam P.,Skrydstrup, Troels
supporting information, p. 5775 - 5778 (2019/08/26)
Bench-stable tablets (COtabs) have been developed for the rapid and safe production of carbon monoxide. The tablets can be made in less than 5 min without the use of a glovebox and only require a stock solution of an amine base to liberate a specific quantity of CO in a two-chamber system. The COtabs were tested in five different carbonylation reactions and provided similar yields compared to literature procedures. Finally, a gram-scale reaction was conducted, as well as 13C-isotope labeling of the anticancer drug, olaparib.
Pyrazole compound containing N-aryl sulfonate and synthesis and application thereof
-
Paragraph 0032, (2018/07/10)
The invention discloses a pyrazole compound containing N-aryl sulfonate. A structural formula of the pyrazole compound is shown in the description. Proofed by pharmacological study, the pyrazole compound has the advantages that the activity of cyclooxygenase 2 is inhibited; the high-efficiency inhibition function on the generation of cyclooxygenase 2 due to inflammation mediums is realized, so that the pyrazole compound can be used as an active matter, and the prepared anti-inflammation medicine can be used for treating the inflammations, such as rheumatic arthritis and rheumatalgia, and the diseases and symptoms, such as fevers.
ARYL BETA DIKETONES AND THEIR USE A ODORANTS
-
Page/Page column 13; 21, (2017/12/09)
The present invention refers to aryl beta diketones of the formula (I) wherein Y, R1, R2 and R3 have the same meaning as given in the description. The invention further refers to fragrance compositions and fragranced articles comprising them.
Syntheses, characterization and antimicrobial evaluation of some 1, 3, 5-trisubustituted pyrazole derivatives
Gautam, Vertika,Chawla, Viney,Sonar, Pankaj K.,Saraf, Shailendra K.
experimental part, p. 1190 - 1195 (2011/12/05)
A series of 1, 3, 5-trisubustituted pyrazole derivatives were synthesized and screened for antimicrobial activity. The compounds (2j-o) were evaluated against two gram-positive and two gram-negative bacteria and one fungus, at concentrations of 10 μg/mL a
A convenient synthesis of 5/7-chloro-4H-1, 4-benzothiazines
Kumar, Gulshan,Gupta, Vandana,Gautam,Gupta
, p. 381 - 384 (2007/10/03)
5/7-Chloro-4H-1,4-benzothiazines have been synthesized by the condensation of sustituted 2-amino-3/5-chlorobenzenethiol with compounds containing active methylene group in dimethylsulfoxide which causes oxidative cyclization via enaminoketone intermediate. The IR, NMR and Mass spectra have been also included.
Multiple Melting Behaviour in Square-planar trans-Bis-(1-p-n-alkylphenylbutane-1,3-dionato)copper(II) - The Effect of Alkyl Chain Length
Ohta, Kazuchika,Jiang, Guang-Jie,Yokoyama, Masaaki,Kusabayashi, Shigekazu,Mikawa, Hiroshi
, p. 283 - 294 (2007/10/02)
The title complexes having different n-alkyl groups from methyl to dodecyl have synthesized.All these complexes exhibit solid polymorphism.The number of polymorphs depends on the length of the alkyl chain: two for n (the number of carbon atoms) = 0-2, three for n = 3-5 and 12, and four for n = 6-11, respectively.Each polymorphic form except those with the highest m.p.s. exhibits multiple melting behaviour: double melting for n = 0-5,8, and 12, and triple melting for n = 6-11 except 8.The m.p.s. of the complexes with alkyl groups of odd carbon atoms are higher than those with even atoms, while the respective ligand solids show the opposit e even-odd effect in their m.p.s.
