56159-89-8Relevant articles and documents
High Chemo-/Stereoselectivity for Synthesis of Polysubstituted Monofluorinated Pyrimidyl Enol Ether Derivatives
Kang, Lei,Wang, Fang,Zhang, Jinlong,Yang, Huameng,Xia, Chungu,Qian, Jinlong,Jiang, Gaoxi
supporting information, p. 1669 - 1674 (2021/03/08)
A novel intramolecular Smiles rearrangement of α-fluoro-β-keto-pyrimidylsulfones (usually used as a carbon nucleophile) was developed, providing a versatile avenue for synthesis of tri/tetra-substituted monofluorinated pyrimidyl enol ethers. Among these, diverse (Z)-monofluorovinylsulfones and sulfinates were efficiently assembled by adding extra electrophile and fine-tuning reaction conditions. The process is triggered by a keto-enol tautomerism from enol oxyanion to pyrimidine 2-carbon, completely different from the classical carbon nucleophilic addition reaction approach.
Utilization of the 1,2,3,5-thiatriazolidin-3-one 1,1-dioxide scaffold in the design of potential inhibitors of human neutrophil proteinase 3
Dou, Dengfeng,He, Guijia,Li, Yi,Lai, Zhong,Wei, Liuqing,Alliston, Kevin R.,Lushington, Gerald H.,Eichhorn, David M.,Groutas, William C.
experimental part, p. 1093 - 1102 (2010/04/24)
The S′ subsites of human neutrophil proteinase 3 (Pr 3) were probed by constructing diverse libraries of compounds based on the 1,2,3,5-thiatriazolidin-3-one 1,1-dioxide using combinational and click chemistry methods. The multiple points of diversity embodied in the heterocyclic scaffold render it well-suited to the exploration of the S′ subsites of Pr 3. Molecular modeling studies suggest that further exploration of the S′ subsites of Pr 3 using the aforementioned heterocyclic scaffold may lead to the identification of highly selective, reversible competitive inhibitors of Pr 3.
Antiproliferative 2-(heteroaryl)-aminothiazole compounds and pharmaceutical compositions, and methods for their use
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Page/Page column 23, (2010/02/10)
Compounds represented by the Formula (I): are described. The compounds and pharmaceutical compositions containing them may be used in inhibiting and/or modulating protein kinases, in treating or preventing diseases associated with protein kinases, and/or in treating or preventing cellular proliferative diseases.