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PYRIMIDINE DERIVATIVES AS CORTICOTROPIN RELEASING FACTOR INHIBITORS

The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) useful for the treatment of depression, anxiety, affective disorders, feeding disorders, post-traumatic stress disorder, headache, drug addiction, inflammatory disorders, drug or alcohol withdrawal symptoms and other conditions the treatment of which can be effected by the antagonism of the CRF-1 receptor. ”

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

Brief introduction of Pd2(DBA)3

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Bromomethyllithium-mediated chemoselective homologation of disulfides to dithioacetals

An efficient, chemoselective homologation of disulfides and diselenides to the corresponding dithio- and diselenoacetals has been developed via the addition of bromomethyllithium. Chemoselectivity is fully preserved in the presence of concomitant electrophilic sites decorating the substrates. The synthetic potential of selected dithioacetals has been evaluated in Feringa-Fananas-Mastral-type Pd-catalyzed coupling with an organolithium and in the unusual 1,4-addition to a Weinreb amide.

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

Archives for Chemistry Experiments of Pd2(DBA)3

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Low-Cost N,N?-Bicarbazole-Based Dopant-Free Hole-Transporting Materials for Large-Area Perovskite Solar Cells

Despite the recent unprecedented development of efficient dopant-free hole transporting materials (HTMs) for high-performance perovskite solar cells (PSCs) on small-area devices (?0.1 cm2), low-cost dopant-free HTMs for large-area PSCs (?1 cm2) with high power conversion efficiencies (PCEs) have rarely been reported. Herein, two novel HTMs, 3,3?,6,6? (or 2,2?,7,7?)-tetrakis(N,N?-di-p-methoxyphenylamine)-N,N?-bicarbazole (3,6 BCz-OMeTAD or 2,7 BCz-OMeTAD), are synthesized via an extremely simple route from very cheap raw materials. Owing to their excellent film-forming abilities and matching energy levels, 3,6 BCz-OMeTAD and 2,7 BCz-OMeTAD can be successfully employed as a perfect ultrathin (?30 nm) hole transporting layer in large-area PSCs up to 1 cm2. The 3,6 BCz-OMeTAD and 2,7 BCz-OMeTAD based large-area PSCs show highest PCEs up to 17.0% and 17.6%, respectively. More importantly, high performance large-area PSCs based on 2,7 BCz-OMeTAD retain 90% of the initial efficiency after 2000 h storage in an ambient environment without encapsulation.

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

Can You Really Do Chemisty Experiments About 1,1′-Bis(diphenylphosphino)ferrocene-palladium(II)dichloride dichloromethane complex

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Pd-catalyzed coupling reaction of allyl and propargyl ethers with chlorosilanes

Pd-catalyzed synthesis of allylsilanes from chlorosilanes and allyl ethers is described. The reaction proceeds efficiently at room temperature by the use of phenyl or vinyl Grignard reagent in the presence of palladium catalysts. The present method can also be applied to synthesis of propargylsilanes by the use of propargyl ethers. Copyright

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

More research is needed about 32005-36-0

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Cyclopropenylidene carbene ligands in palladium catalysed coupling reactions: Carbene ligand rotation and application to the Stille reaction

Reaction of [Pd(PPh3)4] with 1,1-dichloro-2,3- diarylcyclopropenes gives complexes of the type cis-[PdCl2(PPh 3)(C3(Ar)2)] (Ar = Ph 5, Mes 6). Reaction of [Pd(dba)2] with 1,1-dichloro-2,3-diarylcyclopropenes in benzene gave the corresponding binuclear palladium complexes trans-[PdCl2(C 3(Ar)2)]2 (Ar = Ph 7, p-(OMe)C 6H48, p-(F)C6H49). Alternatively, when the reactions were performed in acetonitrile, the complexes trans-[PdCl2(NCMe)(C3(Ar)2)] (Ar = Ph 10, p-(OMe)C6H411 and p-(F)C6H4) 12) were isolated. Addition of phosphine ligands to the binuclear palladium complex 7 or acetonitrile adducts 11 and 12 gave complexes of the type cis-[PdCl 2(PR3)(C3(Ar)2)] (Ar = Ph, R = Cy 13, Ar = p-(OMe)C6H4, R = Ph 14, Ar = p-(F)C 6H4, R = Ph 15). Crystal structures of complexes 6¡¤3.25CHCl3, 10, 11¡¤H2O and 12-15 are reported. DFT calculations of complexes 10-12 indicate the barrier to rotation about the carbene-palladium bond is very low, suggesting limited double bond character in these species. Complexes 5-9 were tested for catalytic activity in C-C coupling (Mizoroki-Heck, Suzuki-Miyaura and, for the first time, Stille reactions) and C-N coupling (Buchwald-Hartwig amination) showing excellent conversion with moderate to high selectivity.

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

A new application about [1,1′-Bis(diphenylphosphino)ferrocene]dichloropalladium(II)

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Synthesis of a novel polycyclic ring scaffold with antimitotic properties via a selective domino Heck-Suzuki reaction

The synthesis of a previously undescribed sp3-rich 6-5-5-6 tetracyclic ring scaffold using a palladium catalysed domino Heck-Suzuki reaction is reported. This reaction is high-yielding, selective for the domino process over the direct Suzuki reaction and tolerant towards a variety of boronic acids. The novel scaffold can also be accessed via domino Heck-Stille and radical cyclisations. Compounds based around this scaffold were found to be effective antimitotic agents in a human cancer cell line. Detailed phenotypic profiling showed that the compounds affected the congression of chromosomes to give mitotic arrest and apoptotic cell death. Thus, a novel structural class of antimitotic agents that does not disrupt the tubulin network has been identified. This journal is

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

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A one-pot, multi-component reaction cascade for the rapid synthesis of diversely functionalized heteroaryl methyl substrates

A novel one-pot, ?green? protocol to rapidly access pharmaceutically relevant heteroaryl methyl substrates is described. This process allows for a tandem SN2/Suzuki-Miyaura reaction or Sonogashira reaction across a breadth of chemical diversity with yields ranging between 31 and 87% for the tandem Suzuki-Miyaura process and 50?66% for the tandem Sonogashira process. This procedure tolerates S, N, and O heteroatom linkers and is amenable for both rapid and robust lead development screening. In addition, T-type and N-type calcium channel blocker (15) was synthesized in 43% yield using this methodology which stands as an improvement in both yield and reaction time of the previously reported synthesis. The one-pot protocol also allows for the inclusion of greater chemical diversity within the scaffold of 15.

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

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Practical one-pot preparation of magnesium Di(hetero)aryl- and magnesium dialkenylboronates for Suzuki-Miyaura cross-coupling reactions

Mg for B: An atom-economical one-pot synthesis by direct magnesium insertion in the presence of B(OBu)3 and LiCl allows a broad range of functionalized (hetero)aryl and alkenyl bromides to be converted into magnesium diorganoboronates 2, which undergo Suzuki-Miyaura cross-coupling reactions with various aryl (pseudo)halides (see scheme). Both aryl groups of 2 are transferred and furnish the products in good to excellent yields. Copyright

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

Final Thoughts on Chemistry for Pd2(DBA)3

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Regioisomerism of an alkyl-substituted bithiophene comonomer in (3: E,8 E)-3,8-bis(2-oxoindolin-3-ylidene)naphtho-[1,2- b:5,6- b ?]difuran-2,7(3 H,8 H)-dione (INDF)-based D-A polymers for organic thin film transistors

Two donor-acceptor (D-A) polymers based on (3E,8E)-3,8-bis(2-oxoindolin-3-ylidene)naphtha-[1,2-b:5,6-b?]difuran 2,7(3H,8H)-dione (INDF) and substituted regioisomeric bithiophene (BT) units with different side chain positions (head-to-head, HH, and tail-to-tail, TT) were synthesized. PINDFBT-(HH) achieved electron (mue) and hole (muh) mobilities as high as 0.33 cm2 V-1 s-1 and 0.15 cm2 V-1 s-1, respectively, while PINDFBT-(TT) showed an order of magnitude lower mobilities with mue of 0.07 cm2 V-1 s-1 and muh of 0.02 cm2 V-1 s-1. The distinctly different electrical performance of these two polymers originates from their different side chain placements on the bithiophene units and consequently different electronic structures, backbone coplanarity, chain packing, and thin film morphology. Our results showed that a bithiophene unit with an HH substitution pattern is much more favoured in terms of the charge transport property of the polymers.

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

Top Picks: new discover of [1,1′-Bis(diphenylphosphino)ferrocene]dichloropalladium(II)

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Ferrocenyl anthracenes: Synthesis and molecular structure

The synthesis of a series of ferrocenylanthracene derivatives is described, utilising the palladium catalysed coupling reaction of 1,1?-bis(chlorozincio)ferrocene with halo-anthracenes. Bis-1,1?-(9-anthracenyl)ferrocene (1) was characterised by single crystal X-ray diffraction and shows an eclipsed ferrocenyl geometry. X-ray crystallographic studies indicate that there are no clear stacking interactions of either an intra-or intermolecular nature between the anthracenyl rings in the structure. A series of 9-and 10-disubstituted ferrocenylanthracene derivatives has also been prepared. In each case the palladium catalyst (Pd(dppf)Cl2) is recovered in a modified form, e.g. as the [(dppf)PdBr(9-anthracenyl)] complex in the synthesis of bis-1,1?-(9-anthracenyl)ferrocene. The single crystal X-ray structure of one such palladium complex [(dppf)PdBr-{9-(10-chloroanthracenyl)}] (15a) has been determined in a case where chloride/bromide exchange had occurred in the palladium complex intermediate. The potential application of compound 1 as synthon for the construction of a molecular sensing device is discussed. Cyclic voltammetry and fluorescence studies have been carried out for selected derivatives.

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