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Trideuteriomethoxylation of aryl and heteroaryl halides

Direct access to trideuteriomethoxylated aromatic and heteroaromatic compounds has been developed. Various aryl and heteroaryl halides underwent d3-methoxylation under mild reaction conditions by using a catalyst system composed of the commercially available monodentate phosphane ligand tBuXPhos and Pd(OAc)2. Inexpensive CD3OD served as an efficient trideuteriomethoxylating agent. The simple and straightforward synthesis of labeled methyl (hetero)aryl ethers via palladium-catalyzed C-O cross-coupling reaction of (hetero)aryl halides with CD3OD was developed. The tBuXPhos ligand is used for the first time in ether synthesis. Copyright

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Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

 

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Palladium-catalysed amination of halopyridines on a KF-alumina surface

Palladium-catalysed C-N hetero cross-coupling reactions between bromopyridines and amines (both primary and secondary) can be efficiently performed on a KF-alumina (basic) surface, thus negating the use of strong bases such as sodium tert-butoxide. The reaction conditions are optimised with reference to catalytic systems, solvents and the surface.

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Hepatitis C Virus Inhibitors

Hepatitis C virus inhibitors having the general formula (I) are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

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Palladium-catalyzed selective decarboxylative coupling reaction versus direct C – H arylation for arylation of heteroaromatics

Conditions for selective palladium-catalyzed decarboxylative 2-arylation of 3-substituted thiophene and furan derivatives bearing an ester at C2 position have been established. By using 2 mol% phosphine-free Pd(OAc)2 as the catalyst and a mixture of KOH and K2CO3 as the bases, in dimethylacetamide, moderate to good yields of the desired 2-arylated products were obtained. A range of functional groups such as nitrile, nitro, formyl or acetyl on the aryl bromides was tolerated. This method allows us to employ in some cases more convenient reactants in terms of cost or physical properties (boiling point) for arylations. Copyright

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Efficient and regioselective access to bis-heterocycles via palladium- catalysed coupling of organostannanes and organozincates derived from C-6 lithiated 2-methoxypyridine

The efficient and regioselective synthesis of various bis-heterocyclic compounds was performed using a regioselective one-pot lithiation- transmetallation-cross-coupling of 2-methoxypyridine.

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Aryl 1-but-3-ynyl-4-phenyl-1,2,3,6-tetrahydropyridines as potential antipsychotic agents: Synthesis and structure-activity relationships

A novel series of aryl 1-but-3-ynyl-4-phenyl-1,2,3,6- tetrahydropyridines with dopaminergic activity is described. The structure- activity relationships of this series were studied by synthesis of analogs and evaluation of their affinities for the dopamine (DA) D2 receptor and inhibition of locomotor activity (LMA) in rodents. The basic amine, alkyne chain length, and aryl groups were varied. Compounds having a 4-phenyl- 1,2,3,6-tetrahydropyridine and an aryl group with hydrogen-bonding substituents separated by a butynyl chain were found to have the most potent dopaminergic activity. Several compounds that were found to have exceptional in vivo activity in LMA inhibition in rodents were evaluated for additional pharmacological activity including binding affinities for other DA receptor subtypes as well as effects on brain DA synthesis, DA neuronal firing, and conditioned avoidance responding in squirrel monkeys.

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Palladium-catalyzed direct arylation of luminescent bis-cyclometalated iridium(III) complexes incorporating C^N- or O^O-coordinating thiophene-based ligands: An efficient method for color tuning

We report the palladium-catalyzed direct 5-arylation of both metalated and nonmetalated thiophene moieties of iridium complexes 2, 3, and 4 with aryl halides via C-H bond functionalization. This method opens new routes to varieties of Ir complexes in only one step, allowing easy modification of the nature of the ligand. The photophysical properties of the new functionalized complexes have been studied by means of absorption and emission spectroscopy. The extension of the pi-conjugated system induces a bathochromic and hyperchromic shift of the absorption spectra, an effect reproduced by first principle calculations. Indeed, the bathochromic shifts are related to a more delocalized nature of the excited-states. All complexes are photoluminescent in the red region of the spectrum. This study establishes that arylation of the thienyl ring affects strongly the electronic properties of the resulting complexes, even when the thienyl ring is remote and not directly metalated to the iridium center, as in the thienyltrifluoroacetonate complex 4.

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Isoquinoline – Wikipedia,
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Three-component coupling of isoquinoline, activated alkyne and nitromethane: A facile synthesis of nitromethyl derivatives of 1,2-dihydroisoquinolines

A three-component coupling (3CC) of isoquinoline, activated alkynes and nitromethane has been achieved for the first time to produce nitromethyl derivatives of dihydroisoquinoline in excellent yields with high selectivity. The reaction proceeds smoothly at 25 C without catalyst. Georg Thieme Verlag Stuttgart.

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NEW PYRIDAZIN-3(2H)-ONE DERIVATIVES

Pyridazin-3(2H)-one derivatives of formula (I) are found to inhibit PDE-4:, wherein R1, R2 and R4 are organic radicals, R3is a cyclic group, and R5 is an ester or an aryl or heteroaryl group.

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Isoquinoline | C9H7N – PubChem

 

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CoCl(PPh3)3 as Cyclotrimerization Catalyst for Functionalized Triynes under Mild Conditions

The ubiquitary Co(I) complex CoCl(PPh3)3 was found to be a convenient catalyst for the [2 + 2 + 2] cycloaddition of functionalized triynes under mild reaction conditions and devoid of any additional additive, yielding the substituted arene compounds. Successful development of synthetic routes to various triynes and the subsequent cyclotrimerization key step gave systematic access to a variety of different bi- and triaryls with good to excellent yields for the cyclization.

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Reference£º
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem