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The present invention relates to a highly enantioselective process for the preparation of enantiomerically pure cyclopentane- and -pentene beta-amino acids of the general formula (I) STR1 in which A and L, A and D or E and L, D and E, R2, R3, T and R1 have the meaning given in the description.

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

Extracurricular laboratory:new discovery of Pd2(DBA)3

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The present invention relates to certain compounds (e.g., imidazopyrazine, imidazopyridine, imidazopyridazine and imidazpyrimidine compounds) that act as inhibitors of the MAP kinase interacting kinases MNK2a, MNK2b, MNK1a, and MNK1b. The present invention further relates to pharmaceutical compositions comprising these compounds, and to the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of diseases (e.g., proliferative diseases (e.g., cancer), inflammatory diseases, Alzheimer’s disease), as well as methods of treating these 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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Three NCN diimine ligands 4-6 were synthesized after condensation of isophthalaldehydes 1-3 and anilines. Treatment of 4-6 with Pd2(dba)3 in toluene resulted in the corresponding PdII-NCN-But (7), PdII-NCN-H (8) and PdII-NCN-NO2 (9) pincer complexes, respectively with high yields. Palladium pincers 7-9 and their precursors 4-6 were fully characterized by elemental analysis, IR, 1H NMR and 13C NMR spectroscopy. The molecular structures of 7b and 9b were also determined by X-ray single crystal diffraction. Sonogashira coupling of phenyl acetylene and 3-nitrobenzene catalyzed by 7-9 show that 9 exhibits the highest catalytic activity, suggesting that the electron withdrawing groups at the position-4 of palladium atom in palladium pincers will enhance their catalytic activity.

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

More research is needed about 1,1′-Bis(diphenylphosphino)ferrocene-palladium(II)dichloride dichloromethane complex

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Selective iodination of the cyclopentadienylruthenium tricarbadecaboranyl complexes 1-(eta5-C5H5)-2-Ph-closo-1,2,3,4- RuC3B7H9 (1) and 1-(eta5-C 5(CH3)5)-2-Ph-closo-1,2,3,4-RuC 3B7H8 (2) to form their mono-iodo derivatives, 1-(eta5-C5H5)-2-Ph-6-I-closo-1,2,3,4-RuC 3B7H9 (3) and 1-(eta5-C 5(CH3)5)-2-Ph-6-I-closo-1,2,3,4-RuC 3B7H8 (4), was achieved in 90% yields by their reactions with ICl in CH2Cl2 solutions. Also isolated in trace amounts from the reaction with 2 was the di-iodo 1-(eta5- C5(CH3)5)-2-Ph-6,11-I2-closo-1,2,3, 4-RuC3B7H7, (5) complex. The sonication-promoted Sonogashira coupling reaction of 3 with terminal acetylenes catalyzed by Pd(dppf)Cl2/CuI yielded the functionalized ruthenatricarbadecaboranyl complexes 1-(eta5-C5H 5)-2-Ph-6-(Ph-C?C)-closo-1,2,3,4-RuC3B 7H8 (6), 1-(eta5-C5H 5)-2-Ph-6-[CH3CH2C(O)OCH2-C?C] -closo-1,2,3,4-RuC3B7H8 (7), 1-(eta5-C5H5)-2-Ph-6-[(eta5- C5H5)Fe(eta5-C5H 4)-C?C]-closo-1,2,3,4-RuC3B7H 8 (8) and 1-(eta5-C5H5)-2-Ph-6- [(CH3)3Si-C?C]-closo-1,2,3,4-RuC3B 7H8 (9). These reactions thus provide a versatile, systematic pathway for the syntheses of a wide variety of new types of functionalized ruthenatricarbadecaboranyl complexes.

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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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The chromenone core is an ubiquitous group in biologically active natural products and has been extensively used in organic synthesis. Fluorine-derived compounds, including those with a trifluoromethyl group (CF 3), have shown enhanced biological activities in numerous pharmaceuticals compared with their non-fluorinated analogues. 2-Trifluoromethylchromenones can be readily functionalized at the 8- and 7-positions, providing chromenones cores of high structural complexity, which are excellent precursors for numerous trifluoromethyl heterocycles.

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

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An iridium-catalyzed site-selective C-H borylation of 2-pyridones has been developed. The site selectivity is predominantly controlled by steric factors, and we can access C4, C5, and C6 C-H on the 2-pyridone ring by the judicious choice of ligand and solvent. Subsequent Suzuki-Miyaura cross-coupling of the borylated products also proceeds to form the corresponding arylated pyridones in good overall yields.

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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 first 3H-1,3-azaphospholo-pyridines 2a-c were synthesized as racemic mixtures in modest to medium yield by the reaction of N-(2-chloropyrid-3-yl)-trimethylacetimidoyl chloride 1 with RPLi2 (R = Ph, n-Bu, i-Bu), generated from RPH2 and BuLi in THF at -70 C, and studied with respect to their suitability as ligands (L) in transition metal complexes. Reactions of 2a with group 6 metal(0) pentacarbonyls led to P-coordinated LM(CO)5 complexes 3a-5a (Cr, Mo, W) and the reaction of 2c with (norbornadiene)Mo(CO)4 surprisingly to 4c. [Rh(1,5-COD)Cl]2 and 2a,b, in metal/ligand ratio 1 : 1, furnished LRh(1,5-COD)Cl complexes 6a,b with P-coordination, 6b accompanied by a minor contamination by the bis-coordinated L[Rh(COD)Cl]2 complex 7b. Reactions of 2a,b with [(allyl)PdCl]2 proceeded in THF with dismutation of N-coordinated (allyl)PdCl and formed with 2a a labile crude product [(2a){(allyl)PdCl}1.2(PdCl2)0.8]·C4H8O, with the composition close to L[Pd(allyl)Cl]PdCl2 THF (8a·THF), which converted during crystallization to 9a, whereas 2b directly formed the N,N?-PdCl2-bridged bis[LPd(allyl)chloride] complex 9b. Conversion of 2b with equimolar amounts of Pd(CH3CN)2Cl2 in THF, or Na2PdCl4 in methanol, gave rise to the dimeric P,N-bridging complex 10b. Crystal structure analyses of 6a (rac), 9b·2CDCl3 (meso), 10b·4.5THF and 10b·2D6-acetone (rac) provided detailed structural information. 10b, but more efficiently complexes formed in situ from 2a,b and Pd2(DBA)3 or Pd(OAc)2, catalysed the arylamination of 2-bromopyridine with 2,4,6-trimethylaniline.

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Reference:
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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A diastereoselective mono-allylation reaction at the alpha-position of symmetric cyclic ketones by using tert-butanesulfinamide as a chiral auxiliary is explored. Excellent yields and high diastereomeric ratios were achieved under palladium(0) catalysis in the presence of a readily available achiral phosphine ligand.

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

Top Picks: new discover of 14871-92-2

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New complexes of 5,6-diamino-4-hydroxy-2-mercaptopyrimidine (Hdahmp), [Zn(Hdahmp)2Cl2], [Zn(bpy)(dahmp)]Cl, [Zn(Hdahmp)2]SO4, [Pd(Hdahmp)(dahmp)]Cl, [Pt(dahmp-H)]+n, [M(bpy)(dahmp]Cl, [M(bpy)(Hdahmp]Cl2 (M(II) = Pd, Pt), [Ru(dahmp)2(PPh3)2], [Rh(dahmp)2(H2O)2]Cl, [Ag2(Hdahmp)2], cis-[MoO2(dahmp?3HCl)2] and cis-[MoO2(Hdahmp)(DMF)Cl]Cl have been synthesized and characterized on the basis of elemental analyses, IR, NMR (1H, 13C, 31P), UV-Vis and ESI-mass spectrometry, thermal and molar conductivity measurements. 5,6-Diamino-4-hydroxy-2-mercaptopyrimidine exhibits five different modes of chelation: (i) a neutral bidentate ligand through the cyclic nitrogen (N-3) and thione sulfur atoms, (ii) a mononegative bidentate ligand through the deprotonated cyclic nitrogen (N-1) and thione sulfur atoms, (iii) a mononegative bidentate ligand through the cyclic nitrogen (N-3) and deprotonated hydroxy centers, (iv) a tetradentate ligand through the cyclic nitrogens (deprotonated N-1, N-3), thione and deprotonated hydroxy oxygen centers, and (v) a mononegative bidentate through the deprotonated cyclic nitrogen (N-3) and ketonic oxygen atoms. The free Hdahmp and several of its complexes have been tested against the human serous ovarian cancer (OV-90) and human ovarian cancer (OVCAR-8) cell lines.

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