1408088-31-2Relevant academic research and scientific papers
Catalytic Friedel–Crafts C?H Borylation of Electron-Rich Arenes: Dramatic Rate Acceleration by Added Alkenes
Yin, Qin,Klare, Hendrik F. T.,Oestreich, Martin
supporting information, p. 3712 - 3717 (2017/03/21)
In the electrophilic C?H borylation of electron-rich aromatic compounds with catecholborane, the catalytic generation of the boron electrophile is initiated by heterolysis of the B?H bond by various Lewis and Br?nsted acids, with a boronium ion formed exclusively. After ligand dissociation, the corresponding borenium ion undergoes regioselective electrophilic aromatic substitution on aniline derivatives as well as nitrogen-containing heterocycles. The catalysis is optimized using B(C6F5)3 as the initiator and proceeds without the addition of an external base or dihydrogen acceptor. Temperatures above 80 °C are generally required to secure efficient turnover in these Friedel–Crafts-type reactions. Mechanistic experiments reveal that regeneration of the boronium/borenium ion with dihydrogen release is rate-determining. This finding finally led to the discovery that, with added alkenes, catalytic C?H borylations can, for the first time, be carried out at room temperature.
SUBSTITUTED PYRIDOPYRAZINES AS NOVEL SYK INHIBITORS
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Paragraph 0187; 0188; 0189, (2014/05/08)
Provided are pyridopyrazine compounds of formula (1), pharmaceutical compositions thereof and methods of use therefore, wherein R1, R2, R3, R4 and m are as defined in the specification.
SUBSTITUTED PYRIDOPYRAZINES AS NOVEL SYK INHIBITORS
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Page/Page column 39, (2013/02/27)
Provided are certain pyridopyrazine compounds, pharmaceutical compositions thereof and methods of use therefor.
NOVEL COMPOUNDS AS MODULATORS OF PROTEIN KINASES
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Page/Page column 115, (2012/11/14)
The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
NOVEL COMPOUNDS AS MODULATORS OF PROTEIN KINASES
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Page/Page column 107, (2012/12/13)
The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
