37860-86-9Relevant articles and documents
The Guareschi-Thorpe Cyclization Revisited - An Efficient Synthesis of Substituted 2,6-Dihydroxypyridines and 2,6-Dichloropyridines
Eriksson, Magnus C.,Zeng, Xingzhong,Xu, Jinghua,Reeves, Diana C.,Busacca, Carl A.,Farina, Vittorio,Senanayake, Chris H.
, p. 1455 - 1460 (2018)
DBU as base is key in a practical modified Guareschi-Thorpe cyclization of β-keto esters and 2-cyanoacetamide to allow the synthesis of substituted pyridones in good to excellent yields. The chlorination of DBU salts of pyridones with POCl 3 in the presence of a quaternary ammonium salt under standard atmospheric reflux conditions as opposed to the typical pressure equipment led to high yields of substituted 2,6-dichloropyridines.
The guareschi pyridine scaffold as a valuable platform for the identification of selective PI3K inhibitors
Galli, Ubaldina,Ciraolo, Elisa,Massarotti, Alberto,Margaria, Jean Piero,Sorba, Giovanni,Hirsch, Emilio,Tron, Gian Cesare
supporting information, p. 17275 - 17287 (2015/12/01)
A novel series of 4-aryl-3-cyano-2-(3-hydroxyphenyl)-6-morpholino-pyridines have been designed as potential phosphatidylinositol-3-kinase (PI3K) inhibitors. The compounds have been synthesized using the Guareschi reaction to prepare the key 4-aryl- 3-cyano-2,6-dihydroxypyridine intermediate. A different selectivity according to the nature of the aryl group has been observed. Compound 9b is a selective inhibitor against the PI3Kα isoform, maintaining a good inhibitory activity. Docking studies were also performed in order to rationalize its profile of selectivity.
CYANOPYRIDINE DERIVATIVE AND USE THEREOF AS MEDICINE
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Page/Page column 8, (2008/06/13)
A therapeutic drug for cancer containing a substance selected from the group consisting of a novel cyanopyridine derivative, a pharmaceutically acceptable salt, a hydrate, a water adduct and a solvate as an active ingredient can be provided.
