852227-90-8Relevant academic research and scientific papers
Naphthalimide-based fluorescent dyes: Impact of extension of φ-conjugation and introduction of an electron-donating moiety on the photophysical properties
Otsuki, Joe,Yamano, Minori,Yamano, Tae,Sugawa, Kosuke
, p. 1506 - 1514 (2018)
Concerning a series of naphthalimide-based fluorescence dyes in which the φ-system is extended with oligothiophene units, it has been revealed that the absorption and fluorescence maxima can be tuned over ca. 100 nm and ca. 180 nm range by extending φ-conjugation, respectively. The effects of the solvent on the fluorescence quantum yield depend on the conjugation length. For the same series but with an electron-donating moiety (push-pull type dyes), the absorption and fluorescence maxima are less dependent on the conjugation length. The fluorescence quantum yields of the push-pull type dyes are large in toluene (>0.3) but extremely low in DMSO. These results will be a guide for the design of naphthalimide-based sensors and probes.
Remote steric control for undirected meta-selective C-H activation of arenes
Asako, Sobi,Ilies, Laurean,Jin, Yushu,Ramadoss, Boobalan
, p. 658 - 663 (2022/02/21)
Regioselective functionalization of arenes remains a challenging problem in organic synthesis. Steric interactions are often used to block sites adjacent to a given substituent, but they do not distinguish the remaining remote sites. We report a strategy
Cobalt-Catalyzed C-F Bond Borylation of Aryl Fluorides
Lim, Soobin,Song, Dalnim,Jeon, Seungwon,Kim, Youngsuk,Kim, Hyunseok,Lee, Sanghee,Cho, Hyungdo,Lee, Byung Chul,Kim, Sang Eun,Kim, Kimoon,Lee, Eunsung
supporting information, p. 7249 - 7252 (2018/11/23)
A mild and practical cobalt-catalyzed defluoroborylation of fluoroarenes is presented for the first time. The method permits straightforward functionalization of fluoroarenes, with high selectivity for borylation of C-F over C-H bonds, and a tolerance for aerobic conditions. Furthermore, two-step 18F-fluorination was achieved for expanding the scope of 18F-positron emission tomography probes.
Catalytic Friedel–Crafts C?H Borylation of Electron-Rich Arenes: Dramatic Rate Acceleration by Added Alkenes
Yin, Qin,Klare, Hendrik F. T.,Oestreich, Martin
, 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.
Catalytic aromatic borylation via in situ-generated borenium species
Kitani, Fumiya,Takita, Ryo,Imahori, Tatsushi,Uchiyama, Masanobu
, p. 158 - 166 (2017/07/28)
We have developed a catalytic direct borylation of arenes via in situ-generated borenium species. The choice of appropriate Lewis base was crucial to achieve the catalytic system. Electron-rich arenes were borylated in a regioselective manner.
PHOSPHOINOSITIDE 3-KINASE INHIBITORS WITH ZINC BINDING MOIETY
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Paragraph 0296; 0469, (2016/10/07)
PROBLEM TO BE SOLVED: To provide phosphoinositide 3-kinase inhibitors with a zinc binding moiety. SOLUTION: There is provided a compound represented by formula (I) in the figure. (X is S, O or the like; Y is CH, N or the like; G1 is optionally substituted N or the like; R1 and R2 are each independently H or the like; C is a substituted heterocycle or the like; B is a linear alkyl or the like; Ra and Rb together with the nitrogen atom coupled to them are morpholino or the like; G2 is an indazole ring or the like; q, r and s are independently from 0 to 1, provided that at least one of them is 1; t is from 0 to 1; n is from 0 to 4; and p is from 0 to 2.) COPYRIGHT: (C)2016,JPOandINPIT
TREATMENT OF CANCERS HAVING K-RAS MUTATIONS
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Paragraph 0551, (2013/05/08)
The present invention provides a method of treating a cancer associated with a K-ras mutation in a subject in need thereof. The method comprises the steps of: (1) identifying a subject with a cancer associated with a K-ras mutation; and (2) administering to the subject (i) an inhibitor of PI3 kinase and (ii) an HDAC inhibitor, wherein the PI3 kinase inhibitor and the HDAC inhibitor are administered in amounts which together are therapeutically effective.
TREATMENT OF CANCERS HAVING K-RAS MUTATIONS
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Page/Page column 221, (2011/11/01)
The present invention provides a method of treating a cancer associated with a K- ras mutation in a subject in need thereof. The method comprises the steps of (1) identifying a subject with a cancer associated with a K-ras mutation; and (2) adminsiterign to the subject (i) an inhibitor of PI3 kinase and (ii) an HDAC inhibitor, wherein the PI3 kinase inhibitor and the HDAC inhibitor are administered in amounts which together are therapeutically effective.
