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A general protocol for the highly efficient synthesis of polyarylated benzene derivatives by multiple Suzuki-Miyaura reactions of polychlorinated benzenes was developed. Using bulky and electron-rich phosphine ligands, up to quantitative yields of the desired compounds were achieved. Moreover, the reactions show good functional group tolerance and allow the employment of sterically demanding boronic acids.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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The high expression of proviral insertion site of Moloney murine leukemia virus kinases (Pim-1, -2, and -3) in cancers, particularly the hematopoietic malignancies, is believed to play a role in promoting cell survival and proliferation while suppressing apoptosis. The three isoforms of Pim protein appear largely redundant in their oncogenic functions. Thus, a pan-Pim kinase inhibitor is highly desirable. However, cell active pan-Pim inhibitors have proven difficult to develop because Pim-2 has a low Km for ATP and therefore requires a very potent inhibitor to effectively block the kinase activity at cellular ATP concentrations. Herein, we report a series of quinazolinone-pyrrolopyrrolones as potent and selective pan-Pim inhibitors. In particular, compound 17 is orally efficacious in a mouse xenograft model (KMS-12 BM) of multiple myeloma, with 93% tumor growth inhibition at 50 mg/kg QD upon oral dosing.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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Four novel molecules, 9-(9,10-diphenylanthracen-3-yl)-9H-carbazole (1), 7-(9,10-diphenylanthracen-3-yl)-7H-benzo[c]carbazole (2), 7-(9,10-diphenylanthracen-3-yl)-7H-benzo[e]pyrido[3,2-b]indole (3), 7-(9,10-diphenyl-2-(7H-benzo[e]pyrido[3,2-b]indol-7-yl)anthracen-6-yl)-7H-benzo[e]pyrido[3,2-b]indole (4), based on 9,10-diphenylanthracene with carbazole derivatives, were designed and synthesized via Buchwald-Hartwig cross-coupling reactions. Multilayer OLED devices were fabricated with the following device structure: ITO/2-TNATA (60 nm)/NPB (20 nm)/alpha,beta-ADN:blue dopant materials (10%, 30 nm)/DNAB (30 nm)/Liq:Al. Among those, the device using 1 exhibited the efficient blue emission with a luminous efficiency of 4.56 cd/A, power efficiency of 1.95 lm/W, an external quantum efficiency of 3.42%, and CIE x,y coordinates of (0.15, 0.17) at 20 mA/cm2, respectively.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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This paper describes the catalytic asymmetric diamination of alkyl dienes using N,N?-di-tert-butylthiadiaziridine 1,1-dioxide in the presence of Pd(0) and a chiral phosphoramidite ligand to give cyclic sulfamides in high yield and high ee. The diamination is also amenable to gram scale.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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Highly efficient, solution-processed, deep-blue fluorescent emitters are urgently required to realize inexpensive organic light-emitting diodes (OLEDs) for full-color displays and lighting applications. Herein, two new bipolar fluorescent emitters: 2-(4-(7-(9,9-dimethylacridin-10(9H)-yl)-9,9-diethyl-9H-fluoren-2-yl)phenyl)-1-phenyl-1H-phenanthro[9,10-d]imidazole (AFpPPI) and 2-(3-(7-(9,9-dimethylacridin-10(9H)-yl)-9,9-diethyl-9H-fluoren-2-yl)phenyl)-1-phenyl-1H-phenanthro[9,10-d]imidazole (AFmPPI) are rationally designed and synthesized. These two are afforded from 9,9-dimethyl-9,10-dihydroacridine (DMACR) as an electron donor and phenylphenanthroimadazole (PPI) as an electron acceptor, using 9,9-diethylfluorene as a spacer with different substitution isomers (para or meta). The photophysical, electrochemical, thermal, and charge-transport properties, as well as the electronic distribution of AFpPPI and AFmPPI are investigated and the results are well supported by density functional theory (DFT) and semi-classical Marcus theory. Interestingly, AFpPPI and AFmPPI display deep-blue emission with high fluorescence quantum yields (PhiF). Furthermore, solution-processed, non-doped OLEDs were fabricated with AFpPPI and AFmPPI as an emitter, in which AFpPPI delivered a maximum external quantum efficiency (EQE) of 5.76% with Commission Internationale de l’Eclairage (CIE) coordinates of (0.15, 0.10) and a maximum current efficiency (CE) of 5.39 cd A?1, which is the best performance for deep-blue, solution-processed fluorescent OLEDs based on non-doped bipolar emitters.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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A palladium(II)-catalyzed, copper(I)-mediated Liebeskind-Srogl cross-coupling for the C-6 arylation/alkenylation on purine scaffold is reported. Various boronic acids reacted readily with 8-substituted 6-thiophenylpurines. Georg Thieme Verlag Stuttgart. New York.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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A palladium-catalyzed dearomative syn-1,4-oxyamination protocol using non-activated arenes has been developed. This one-pot procedure utilizes arenophile chemistry, and the corresponding para-cycloadducts are treated with oxygen nucleophiles via formal allylic substitution, providing direct access to syn-1,4-oxyaminated products. The reaction conditions permit a range of arenes, as well as different O-nucleophiles, such as oximes and benzyl alcohols. Moreover, this process was established in an asymmetric fashion, delivering products with high enantioselectivity. The dearomatized products are amenable to a multitude of further derivatizations ranging from olefin chemistry to C?H activation, giving rise to a diverse set of new functionalities. Overall, this dearomative functionalization offers rapid and controlled formation of molecular complexity, enabling straightforward access to functionalized small molecules from simple and readily available arenes.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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The present invention relates to novel compounds which are inhibitors of CRAC channel activity. This invention also relates to pharmaceutical compositions containing them, process for their preparation and their use in therapy.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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This invention concerns heterocyclic derivatives of formula (I) which are useful in inhibiting oxido-squalene cyclase, processes for their preparation and pharmaceutical compositions containing them. The present invention is also concerned with heterocyclic derivatives capable of inhibiting cholesterol biosynthesis and hence the lowering cholesterol levels in blood plasma. The present invention also relates to methods of using such heterocyclic derivatives in diseases and medical conditions such as hypercholesterolemia and atherosclerosis.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method