676501-89-6Relevant articles and documents
C-H Borylation Catalysis of Heteroaromatics by a Rhenium Boryl Polyhydride
Donnelly, Liam J.,Faber, Teresa,Morrison, Carole A.,Nichol, Gary S.,Thomas, Stephen P.,Love, Jason B.
, p. 7394 - 7400 (2021/06/30)
Transition metal complexes bearing metal-boron bonds are of particular relevance to catalytic C-H borylation reactions, with iridium polyboryl and polyhydrido-boryl complexes the current benchmark catalysts for these transformations. Herein, we demonstrate that polyhydride boryl phosphine rhenium complexes are accessible and catalyze the C-H borylation of heteroaromatic substrates. Reaction of [K(DME)(18-c-6)][ReH4(Bpin)(ν2-HBpin)(κ2-H2Bpin)] 1 with 1,3-bis(diphenylphosphino)propane (dppp) produced [K(18-c-6)][ReH4(ν2-HBpin)(dppp)] 2 through substitution of two equivalents of HBpin, and protonation of 2 formed the neutral complex [ReH6(Bpin)(dppp)] 3. Combined X-ray crystallographic and DFT studies show that 2 is best described as a σ-borane complex, whereas 3 is a boryl complex. Significantly, the boryl complex 3 acted as a catalyst for the C(sp2)-H borylation of a variety of heteroarenes (14 examples including furan, thiophene, pyrrole and indole derivatives) and displayed similar reactivity to the iridium analogues.
FIVE- AND SIX-MEMBERED AZA-AROMATIC COMPOUND, PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION, AND APPLICATION
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Paragraph 0088, (2020/04/02)
The invention relates to the field of medicinal chemistry, and to five-membered-fused-six-membered aza-aromatic ring compound, preparation method thereof, pharmaceutical composition and application thereof. In particular, the invention relates to a type o
NOVEL TRICYCLIC COMPOUNDS
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Page/Page column 98; 99, (2019/05/15)
This invention relates to certain novel tricyclic compounds as bromodomain and extra-terminal (BET) inhibitors, their synthesis and their use for treating diseases. More particularly, this invention is directed to fused heterocyclic derivatives useful as
Iridium(I)-Catalyzed C?H Borylation in Air by Using Mechanochemistry
Pang, Yadong,Ishiyama, Tatsuo,Kubota, Koji,Ito, Hajime
supporting information, p. 4654 - 4659 (2019/03/17)
Mechanochemistry has been applied for the first time to an iridium(I)-catalyzed C?H borylation reaction. By using either none or just a catalytic amount of a liquid, the mechanochemical C?H borylation of a series of heteroaromatic compounds proceeded in air to afford the corresponding arylboronates in good-to-excellent yields. A one-pot mechanochemical C?H borylation/Suzuki–Miyaura cross-coupling sequence for the direct synthesis of 2-aryl indole derivatives is also described. The present study constitutes an important milestone towards the development of industrially attractive solvent-free C?H bond functionalization processes in air.
3-(PYRIDIN-3-YL)-ACRYLAMIDE AND N-(PYRIDIN-3-YL)-ACRYLAMIDE DERIVATIVES AND THEIR USE AS PAK OR NAMPT MODULATORS
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, (2017/03/14)
The invention generally relates to cyclic compounds and, more particularly, to a compound represented by Structural Formula I: or a pharmaceutically acceptable salt thereof and pharmaceutical compositions comprising the multicyclic compounds. The invention also relates to a method for treating a disease or disorder selected from cancer (e.g., lymphoma, such as mantle cell lymphoma), a neurodegenerative disease, an inflammatory diseases or an immune system disease (e.g., a T- Cell mediated autoimmune diseases) in a subject in need thereof. The method comprises administering to a subject in need thereof a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof, or a composition comprising a compound of the invention, or a pharmaceutically acceptable salt thereof.
Sterically controlled iodination of arenes via iridium-catalyzed C-H borylation
Partridge, Benjamin M.,Hartwig, John F.
supporting information, p. 140 - 143 (2013/03/28)
A mild method to prepare aryl and heteroaryl iodides by sequential C-H borylation and iodination is reported. The regioselectivity of this process is controlled by steric effects on the C-H borylation step and is complementary to existing methods to form aryl iodides. The iodination of boronic esters has potential for the synthesis of radiolabeled aryl iodides, as demonstrated by the concise synthesis of a potential tracer for SPECT imaging.
A C-H borylation approach to suzuki-miyaura coupling of typically unstable 2-heteroaryl and polyfluorophenyl boronates
Robbins, Daniel W.,Hartwig, John F.
supporting information; experimental part, p. 4266 - 4269 (2012/10/08)
A method for the synthesis of biaryls and heterobiaryls from arenes and haloarenes without the intermediacy of unstable boronic acids is described. Pinacol boronate esters that are analogous to unstable boronic acids are formed in high yield by iridium-catalyzed C-H borylation of heteroarenes and fluoroarenes. These boronates are stable in the solid state or in solution and can be generated and used in situ. They couple with aryl halides in the presence of simple palladium catalysts, providing a convenient route to biaryl and heteroaryl products that have been challenging to prepare via boronic acids.
Iridium-Catalyzed Direct Borylation of Five-Membered Heteroarenes by Bis(pinacolato)diboron: Regioselective, Stoichiometric, and Room Temperature Reactions
Ishiyama, Tatsuo,Takagi, Jun,Yonekawa, Yuhei,Hartwig, John F.,Miyaura, Norio
, p. 1103 - 1106 (2007/10/03)
An iridium(I) complex generated from 1/ 2[Ir(OMe)(COD)]2 and 4,4′-di-tert-butyl-2,2′-bipyridine catalyzed the direct borylation of 2-substituted thiophenes, furans and pyrroles in stoichiometric amounts relative to bis(pinacolato)diboron in hex
