Two metal-free, formal [2 + 2 + 2] cycloaddition strategies for the construction of polycyclic pyridine derivatives are described that proceed via pericyclic cascade mechanisms featuring the participation of unactivated cyano groups as enophile and dienophile cycloaddition partners.

Economic and environmentally friendly bio-mimetic one-pot three and four-component Knoevenagel-hydrogenation (K-H), five-component Knoevenagel-hydrogenation-alkylation (K-H-A) and six-component Knoevenagel-hydrogenation-alkylation-Huisgen cycloaddition (K-H-A-HC) reactions of aldehydes, CH-acids, o-phenylenediamine, alkyl halides and azides using proline, proline-metal carbonate and proline-met...

Bicyclo[2.1.1]hexanes (BCHs) represent an intriguing class of structurally rigid hydrocarbons that can serve as the bioisosteres benzenoids in medicinal chemistry. Methods for synthesis BCHs are, however, limiting. Reported herein is a facile via strain-release-driven [2π + 2σ] cycloaddition bicyclo[1.1.0]butanes (BCBs) with alkenes facilitated by pyridine-boryl radical catalyst. The mild react...

Advances in the fields of proteomics, molecular imaging, and therapeutics are closely linked to the availability of affinity reagents that selectively recognize their biological targets. Here we present a review of Iterative Peptide In Situ Click Chemistry (IPISC), a novel screening technology for designing peptide multiligands with high affinity and specificity. This technology builds upon in ...

The nickel-catalyzed intramolecular cycloaddition of dienes with unactivatable alkynes is found to proceed under mild conditions while the corresponding Diels-Alder cycloaddition of the same substrates either fails or occurs only under forcing conditions. The nickel-catalyzed cycloaddition is also shown to occur with retention of stereochemistry and is not significantly influenced by electronic...

Breast and prostate cancers are a major cause of death each year. Most available anticancer drugs not very effective can side effects. Identifying safe alternative drug with fewer effects for long-term therapy is therefore necessary. The present study was aimed at synthesizing 1,2,3-triazole derivatives evaluating their activity against human breast cancer (MCF-7) (PC-3) cell lines. Novel serie...

Cycloaddition is a fundamental transformation, featuring the assembly of complex cyclic molecules with multiple stereocenters. We report here silver-catalyzed [3+2]-cycloaddition 2,3-disubstituted cyclobutenones an array azomethine ylide...

5-(Octa-1,7-diynyl)-2'-deoxyuridine was converted into the furano-dU derivative 7 by copper-catalyzed cyclization; the pyrolodC-derivative 3 was formed upon ammonolysis. The bicyclic nucleosides 3 and 7 as well as the corresponding non-cyclic precursors 4 and 6 all containing terminal C[triple bond]C bonds were conjugated with the non-fluorescent 3-azido-7-hydroxycoumarin 5 employing the copper...

The facile syntheses of ring-expanded N-heterocyclic carbene (RE-NHC) copper(I) halide complexes are reported. method makes use a weak inorganic base in green solvent. reaction times can be greatly reduced by this weak-base route under microwave irradiation. easy access to these permits an evaluation the catalytic activity and profiling [Cu(RE-NHC)X] Huisgen 1,3-cycloaddition reaction.