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The NF-kappaB family of transcription factors plays an important role in determining cell survival during immune, inflammatory, and stress responses. NF-kappaB activity is frequently deregulated in human cancers and is implicated in the resistance of tumor cells to diverse anticancer agents. We studied the effects of novel analogs of precursors of the… (More)
Pd/C-mediated alkynylation of 5-iodo-pyrazole-4-carboxylic acid, involving the first regioselective construction of α-pyrone ring on a pyrazol moiety via tandem coupling-cyclization process, has been developed to afford pyrano[4,3-c]pyrazol-4(1H)-one in a single pot.
The coupling reaction of o-iodobenzoic acid with terminal alkynes by using a catalyst system of 10% Pd/C-Et3N-CuI-PPh3 has been studied in a variety of solvents. 3-Substituted isocoumarins were formed in good yields and with good regioselectivity when the reaction was performed in EtOH.
[reaction: see text] We herein report a new synthesis of 2-(hetero)aryl-substituted pyridines via heteroarylation of arenes/heteroarenes through AlCl(3)-induced C-C bond-forming reactions. 2-Halopyridines bearing an electron-withdrawing group were reacted with a number of (hetero)arenes to give 2-aryl/heteroaryl-substituted pyridines in good yields.
We herein report the efficient syntheses of 4-(hetero)aryl-substituted 1-chlorophthalazines via heteroarylation of arenes/heteroarenes through AlCl(3)-induced C[bond]C formation reactions. A number of (hetero)arenes were reacted with 1,4-dichlorophthalazine to give aryl/heteroaryl-substituted phthalazines in good to excellent yields. Many of them were… (More)
The metal-free, direct conversion of readily available proline derivatives into 2-aryl-3-iodopyrrolidines is carried out under mild conditions and in good yields, using a sequential radical decarboxylation-oxidation-iodination-arylation reaction. These iodinated pyrrolidines are valuable precursors of other compounds. For instance, they can be cyclized to… (More)
A two-step process for the transformation of readily available carbohydrate derivatives into acyclic C-nucleosides is described. The carbohydrate undergoes a scission process that is followed by the addition of aryl ketone derivatives, allowing the introduction of a variety of aryl rings. The resulting acyclic C-nucleosides are transformed into 2-deoxy… (More)
A new one-pot reaction for the regioselective construction of a six-membered fused N-heterocyclic ring leading to isoquinolones under Pd/C-Cu catalysis is described.