- Preparation method of alpelisib
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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.
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Paragraph 0112-0114
(2021/07/01)
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- Novel synthesis method of PI3K inhibitor Alpelisib
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The invention relates to a novel synthesis method of a PI3K inhibitor Alpelisib. According to the synthesis method disclosed by the invention, the target molecule can be synthesized through four stepsof reactions including one-step substitution reaction of starting raw materials, amino protection group removal and two times of halogenation reaction, the total yield is high, the cost is low, and the HPLC purity of the product reaches 99.5% or above.
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Paragraph 0049-0060
(2020/05/05)
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- Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation
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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.
- 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
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p. 3741 - 3748
(2013/07/27)
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- A CRYSTALLINE FORM 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 AND ITS USE AS PI3K INHIBITOR
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The present invention relates to specific solid forms of (S)-pyrrolidine-l,2-dicarboxylic acid 2-amide l-(4-methyI-5-[2-(2,2,2-trifluoro-l,l-dimethyl-ethyl)-pyridin-4-yl]-thiazol-2-yl)-amide, (I), and its hydrates and 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.
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Page/Page column 33=34
(2012/02/15)
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- 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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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.
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Page/Page column 27
(2013/02/28)
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