1357476-68-6Relevant articles and documents
Preparation method of alpelisib
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Paragraph 0112-0114, (2021/07/01)
The invention provides a preparation method of alpelisib. 2-pyrrole methyl formate and N, N-carbonyldiimidazole which are used as raw materials are subjected to an amidation reaction, a suzuki reaction and an aminolysis reaction to obtain the compound apenelisib shown in the formula I. The method is mild in reaction condition, simple and convenient in treatment, environment-friendly, low in cost and suitable for industrial mass production.
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.