10397-13-4Relevant articles and documents
Regioselective 2-Amination of Polychloropyrimidines
Smith, Sean M.,Buchwald, Stephen L.
, p. 2180 - 2183 (2016)
The regioselective amination of substituted di- and trichloropyrimidines affording the 2-substituted products is reported. While aryl- and heteroarylamines require the use of a dialkylbiarylphosphine-derived palladium catalyst for high efficiency, more nucleophilic dialkylamines produce 2-aminopyrimidines under noncatalyzed SNAr conditions. The key is the use of 5-trimethylsilyl-2,4-dichloropyrimidine as a surrogate for the parent dichloropyrimidine. For more challenging cases, the 2-chloro-4-thiomethoxy analogues were prepared and exclusively afford the desired 2-aminated-4-thiomethoxypyrimidine products.
Discovery of Novel Dual Poly(ADP-ribose)polymerase and Phosphoinositide 3-Kinase Inhibitors as a Promising Strategy for Cancer Therapy
Wang, Junwei,Li, Hui,He, Guangchao,Chu, Zhaoxing,Peng, Kewen,Ge, Yiran,Zhu, Qihua,Xu, Yungen
, p. 122 - 139 (2020)
Concomitant inhibition of PARP and PI3K pathways has been recognized as a promising strategy for cancer therapy, which may expand the clinical utility of PARP inhibitors. Herein, we report the discovery of dual PARP/PI3K inhibitors that merge the pharmaco
PARP-1 and PI3K double-target inhibitor containing benzofuran
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Paragraph 0120; 0122-0123, (2019/06/08)
The invention relates to the field of medicinal chemistry, in particular to a PARP-1 and PI3K double-target inhibitor containing a benzofuran structure (I) (the formula I is shown in the description),a preparation method and a medicine composition containing thereof. Proved by a pharmacodynamic test, the PARP-1 and PI3K double-target inhibitor has the anti-tumor effect.
PI3K INHIBITOR, AND PHARMACEUTICALLY ACCEPTABLE SALT, POLYCRYSTALLINE FORM, AND APPLICATION THEREOF
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Paragraph 0384; 0385; 0386, (2019/06/07)
The present invention relates to a PI3K inhibitor, and a pharmaceutically acceptable salt, polycrystalline form, and application thereof. The invention specifically provides a polycrystalline form of 4-chloro-5-(6-(1-(methylsulfonyl)cyclopropyl)-2-morpholinopyrimidin-4-yl)pyridin-2-amine, a pharmaceutically acceptable salt thereof, or a polycrystalline form of the salt. The invention further discloses a pharmaceutical composition comprising the inhibitor and an application of the pharmaceutical composition.