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S1, 1 ‘-bis (diphenylphosphine) ferrocene dipalladium dichloride is added to a heating device, and the reaction liquid, 1, 1′ -bis (diphenylphosphine) ferrocene dipalladium dichloride is added to the extraction device. S2, and a heating device, a heating reflux 1, and an extraction device are added into the extraction solution after the reaction is finished; and S3, a heating device is added to the extraction solution and the extraction liquid is added into the flask, and stirred, and then the mixture 1 is stirred to obtain a 1’ . method, and a method for preparing the methylene dichloride 5 – 10 ml methylene chloride complex is obtained by the preparation method disclosed by the invention in the following step: 1. S4. 1 – 10h-bis (diphenylphosphine) ferrocene dipalladium chloride 1 complex crystal is obtained by adding an extracting 1 solution 1, and an extracting solution is added into the extraction device through a 0.8 1 condensation 1 – 1.2 pipe; and a heating device is obtained. The method comprises the steps: preparing a filter paper tube, and heating and refluxing the mixture. (by machine translation)

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

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Reactions of sodium tetraarylborates and arylboronic acids with acyl chlorides in the presence of palladium salts afford non-symmetrical ketones in high yields under mild conditions.

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

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Compounds of formula (I) described herein are useful for inhibiting phosphoinositide 3-kinases (PI3K) and the treatment of disorders associated with PI3K enzymes.

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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 key step in accessing the title species (5), the first nonbenzenoid diisocyanobiaryl, involved an unexpected homocoupling of a 6-bromoazulene derivative. The reversible 2e- reduction of 5 was addressed electrochemically and computationally. The shifts in energies of the S 0?S1 and S0?S2 transitions for a series of related 6,6?-biazulenyl derivatives correlate with the e–donating/-withdrawing strength of their 2,2?-substituents but follow opposite trends. Species 5 adsorbs end-on (eta1) to the Au(111) surface via one of its -NC groups to form a 2-nm-thick film. In addition, bimetallic coordination of 5’s -NC termini can be readily achieved.

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

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Palladium complex PdCl2(dppf) and nickel complex NiCl2(dppe) catalyze cross-coupling of unsaturated aryloxy carbohydrates with phenylmagnesium bromide. The nickel catalyst leads to inversion of configuration at the anomeric center while only retention occurs in the case of the palladium catalyst. This quite unusal retention is probably due to the influence of the ring oxygen atom.

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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 novel and direct synthesis of various 2-aminobenzo[b]thiophenes has been developed. The reactions were catalyzed by a combination of Pd(dppf)Cl2 and dppf using odorless and cheap Na2S2O3 as the sulfur source. This strategy allowed us to synthesize important 2-aminobenzo[b]thiophene scaffold more efficiently and conveniently.

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

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Signaling pathways intersecting with the p21-activated kinases (PAKs) play important roles in tumorigenesis and cancer progression. By recognizing that the limitations of FRAX1036 (1) were chiefly associated with the highly basic amine it contained, we devised a mitigation strategy to address several issues such as hERG activity. The 5-amino-1,3-dioxanyl moiety was identified as an effective means of reducing pKa and logP simultaneously. When positioned properly within the scaffold, this group conferred several benefits including potency, pharmacokinetics, and selectivity. Mouse xenograft PK/PD studies were carried out using an advanced compound, G-5555 (12), derived from this approach. These studies concluded that dose-dependent pathway modulation was achievable and paves the way for further in vivo investigations of PAK1 function in cancer and other diseases.

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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 synthesis of tris{5?-[methylbis(2-thienyl)silyl]2,2?- bithienyl-5-yl} methylsilane, a first-generation bithiophenesilane dendrimer, is described. The conditions of effective formation of methyltrithienylsilane were found; methyltris(5-bromo-2-thienyl)silane and a number of other monofunctional derivatives of methyltrithienylsilane were synthesized for the first time. The advantages and drawbacks of the Suzuki and Kumada reactions for the formation of bithienyl fragments in the synthesis of oligothienylsilane dendrimers are discussed.

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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 structure-activity relationship for nitrile-based cruzain inhibitors incorporating a P2 amide replacement based on trifluoroethylamine was explored by deconstruction of a published series of inhibitors. It was demonstrated that the P3 biphenyl substituent present in the published inhibitor structures could be truncated to phenyl with only a small loss of affinity. The effects of inverting the configuration of the P2 amide replacement and linking a benzyl substituent at P1 were observed to be strongly nonadditive. We show that plotting affinity against molecular size provides a means to visualize both the molecular size efficiency of structural transformations and the nonadditivity in the structure-activity relationship. We also show how the relationship between affinity and lipophilicity, measured by high-performance liquid chromatography with an immobilized artificial membrane stationary phase, may be used to normalize affinity with respect to lipophilicity.

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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 Suzuki-Miyaura reaction is a cornerstone method for sp2-sp2 cross-coupling in industry. There has been a concerted effort to enable the use of Ni catalysis as an alternative to Pd in order to mitigate cost and improve sustainability. Despite significant advances, ligand development for Ni-catalyzed Suzuki-Miyaura cross-coupling remains underdeveloped when compared to Pd and, as a consequence, ligands for Ni-catalyzed processes are typically taken from the Pd arena. In this study we evaluate the effect of using a similar Ni and Pd precatalyst based on a common bidentate ligand (dppf) in a head-to-head format for the most common type of biaryl couplings, establishing the practical implications of direct replacement of Pd with Ni, and identifying the potential origins of these observations in a mechanistic context.

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