69214-33-1Relevant articles and documents
SUBSTITUTED FUSED AROMATIC RING DERIVATIVE, COMPOSITION AND USE THEREOF
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Paragraph 0152-0154, (2021/11/04)
Provided are a substituted fused aromatic ring derivative, a composition containing the compound, and a use thereof. The substituted fused aromatic ring derivative is a compound represented by formula (I) or a tautomer, stereoisomer, prodrug, crystal form, pharmaceutically acceptable salt, hydrate or solvate thereof. The compound and the composition can be used to treat various protein tyrosine kinase-mediated diseases or disorders.
Selective Halogenation of Pyridines Using Designed Phosphine Reagents
Alegre-Requena, Juan V.,Levy, Jeffrey N.,Liu, Renrong,McNally, Andrew,Paton, Robert S.
supporting information, p. 11295 - 11305 (2020/07/13)
Halopyridines are key building blocks for synthesizing pharmaceuticals, agrochemicals, and ligands for metal complexes, but strategies to selectively halogenate pyridine C-H precursors are lacking. We designed a set of heterocyclic phosphines that are installed at the 4-position of pyridines as phosphonium salts and then displaced with halide nucleophiles. A broad range of unactivated pyridines can be halogenated, and the method is viable for late-stage halogenation of complex pharmaceuticals. Computational studies indicate that C-halogen bond formation occurs via an SNAr pathway, and phosphine elimination is the rate-determining step. Steric interactions during C-P bond cleavage account for differences in reactivity between 2- and 3-substituted pyridines.
Alkynyl (hetero) aromatic compounds for inhibiting activity of protein kinase
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Paragraph 0590; 0593-0595, (2019/10/07)
The invention relates to alkynyl (hetero) aromatic compounds for inhibiting activity of protein tyrosine kinase. The invention further relates to a pharmaceutical composition containing the alkynyl (hetero) aromatic compounds, and preparation and application of the alkynyl (hetero) aromatic compounds. Specifically, the invention discloses the alkynyl (hetero) aromatic compound shown in an equation (I) and pharmaceutically acceptable salts, stereoisomers, solvates, hydrates, crystal forms, prodrugs and isotopic variants of the alkynyl (hetero) aromatic compound shown in the equation (I). The alkynyl (hetero) aromatic compounds can be used for treating and/or preventing protein tyrosine kinase-related diseases, such as preventing tumors.