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%.
Preparation method and use of thiophene compound
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Paragraph 0105; 0106, (2020/02/17)
The invention belongs to the technical field of pharmaceutical chemistry, and relates to thiophene compounds shown by general formula I, pharmaceutically acceptable salts, solvates or prodrugs and preparation methods thereof. In which substituents L, Ar, R have the meanings given in the specification. The invention also relates to a strong PI3K inhibitory effect of a compound of the general formula I, and also relates to the use of such compounds and pharmaceutically acceptable salts, solvates or prodrugs thereof in the preparation of drugs for the treatment and/or prevention of diseases caused by abnormally high expression of PI3K, in particular in the preparation of drugs for the treatment and/or prevention of cancer.
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.