1357476-67-5Relevant articles and documents
Trifluoromethylation reaction on dimethyl substituted heterocyclic compound
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Paragraph 0044-0061, (2020/12/14)
The invention relates to a method for introducing a trifluoromethyl group through a trifluoromethylation reaction. A trifluoromethylation reagent used in the method is a Umemoto reagent, and a substrate is a wide dimethyl substituent-containing compound. The method has the advantages that the universality of the substrate is reflected, the reaction sites of the substrate acted by the Umemoto reagent in the past are always on the ring, and the site of the trifluoromethylation action is carbon on the dimethyl chain, which is a leap and breakthrough in the richness selection of the substrate andthe trifluoromethylation reaction.
Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation
Furet, Pascal,Guagnano, Vito,Fairhurst, Robin A.,Imbach-Weese, Patricia,Bruce, Ian,Knapp, Mark,Fritsch, Christine,Blasco, Francesca,Blanz, Joachim,Aichholz, Reiner,Hamon, Jacques,Fabbro, Doriano,Caravatti, Giorgio
, p. 3741 - 3748 (2013/07/27)
Phosphatidylinositol-3-kinase α (PI3Kα) is a therapeutic target of high interest in anticancer drug research. On the basis of a binding model rationalizing the high selectivity and potency of a particular series of 2-aminothiazole compounds in inhibiting PI3Kα, a medicinal chemistry program has led to the discovery of the clinical candidate NVP-BYL719.
POLYMORPHS OF (S)-PYRROLIDINE-1,2-DICARBOXYLIC ACID 2-AMIDE 1-({4-METHYL-5-[2-(2,2,2-TRIFLUORO-1,1-DIMETHYL-ETHYL)-PYRIDIN-4-YL]-THIAZOL-2-YL}-AMIDE
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Page/Page column 27, (2013/02/28)
The present invention relates to specific solid forms of (S)-pyrrolidine-1,2- dicarboxylic acid 2-amide l-(4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)-pyridin-4- yl]-thiazol-2-yl)-amide, and its solvates. The present invention further relates to processes for preparing said solid forms, pharmaceutical compositions comprising said solid forms, and methods of using said solid forms and pharmaceutical compositions to treat disease.