5147-80-8Relevant articles and documents
Synthesis of Polysubstituted Pyrimidines from Ketene Dithioacetals Using KF/Al2O3 Catalyst
Yu, Shen-Yi,Cai, Ya-Xian
, p. 3989 - 3995 (2003)
KF/Al2O3 was first used to catalyze the synthesis of 2-alkylthio-4-amino-5-cyano-6-methylthiopyrimidines 3a-f via the reaction of the ketene dithioacetals 1 (prepared from malononitrile) with isothiuronium salts 2a-f. Six pyrimidine compounds were prepared and all of their structures were confirmed by elemental analysis, 1H NMR, and IR. The reaction conditions (solvents, catalyst amounts, and temperature) were investigated for the first time. The separation yield reached 89%.
Discovery and optimization of pyrazolopyrimidine sulfamates as ATG7 inhibitors
Adhikari, Sharmila,Brownell, James E.,Calderwood, Emily F.,Chouitar, Jouhara,D'Amore, Natalie Roy,England, Dylan B.,Foley, Klaudia,Gould, Alexandra E.,Harrison, Sean J.,Huang, Shih-Chung,LeRoy, Patrick J.,Lok, David,Lublinsky, Anna,Ma, Li-Ting,Menon, Saurabh,Yang, Yu,Zhang, Ji
, (2020/08/13)
Autophagy is postulated to be required by cancer cells to survive periods of metabolic and/or hypoxic stress. ATG7 is the E1 enzyme that is required for activation of Ubl conjugation pathways involved in autophagosome formation. This article describes the design and optimization of pyrazolopyrimidine sulfamate compounds as potent and selective inhibitors of ATG7. Cellular levels of the autophagy markers, LC3B and NBR1, are regulated following treatment with these compounds.
Tailored-design Synthesis of Sulfapyrimidine Derivatives
Azzam, Rasha A.
, p. 619 - 627 (2019/01/04)
In this paper, we report an efficient and convenient approach for the synthesis of tailored-design target sulfapyrimidine derivatives expected to show remarkable antimicrobial activities. The approach is based on reacting arylsulfonyl guanidine with α,β-unsaturated carbonyl compounds to afford N-(4,6-diarylpyrimidin-2-yl)arylsulfonamide or with ylidene derivatives to afford N-(6-aryl-5-cyanopyrimidin-2-yl)arylsulfonamide, N-(4-amino-5-cyano-6-(methylthio)-pyrimidin-2-yl)-arylsulfonamide, and N-(5-cyanopyrimidin-2-yl)arylsulfonamide compounds through Michael addition reaction. The structure of the newly synthesized compounds was confirmed from spectral data and elemental analysis.