Herein, we report an unprecedented, short and diastereo-selective synthesis of newly reported aza-diketopiperazine (aza-DKP) scaffolds starting from amino acids. The strategy is based on a Rh(I)-catalyzed hydroformylative cyclohydrocarbonylation of allyl-substituted aza-DKP, followed by a diastereoselective functionalization of the platform. This methodology allows the synthesis of novel bicycl...

The utility of the tethered aminohydroxylation (TA) has been demonstrated by synthesis of the complex β-amino acid residue of microsclerodermins A and B. The TA provided a regio- and stereoselective functionalization of a complex homoallylic alcohol. The route includes late-stage introduction of the aliphatic side chain via a cuprate addition and cross metathesis, a tactic designed to render th...

A methyl ketone, an aryl bromide, an electrophile, and ammonium chloride were combined in a four-component, three-step, and one-pot coupling procedure to furnish substituted isoquinolines in overall yields of up to 80%. This protocol utilizes the palladium catalyzed α-arylation reaction of an enolate, followed by in situ trapping with an electrophile, and aromatization with ammonium chloride. t...

Degradable, cationic poly(β-amino ester)s (PBAEs) with alkyl side chains are developed for non-viral gene delivery. Nanoparticles formed from these PBAE terpolymers exhibit significantly enhanced DNA transfection potency and resistance to aggregation. These hydrophobic PBAE terpolymers, but not PBAEs lacking alkyl side chains, support interaction with PEG-lipid conjugates, facilitating their fu...

As the most studied two-dimensional material, graphene is still attracting a lot of attention from both academia and industry due to its fantastic properties such as lightness, excellent mechanical strength, high conductivity heat electricity. an important branch materials, nanoplatelets show numerous applications in coating, fillers polymer composites, energy conversion storage devices, sensin...

Herein, we report a simple and convenient procedure to prepare para-disubstituted [2.2]paracyclophanes in straightforward manner. Our approach relies on regioselective formylation of N-substituted 4-amino[2.2]paracyclophanes, which allows an easy access series products incorporating reactive aldehyde function para the electron-donating group. These compounds can be engaged variety orthogonal la...

Widely used reagents in the peptide functionalization toolbox, Michael acceptors and N-hydroxysuccinimide (NHS) activated esters, are combined NHS-activated acrylamides for efficient chemoselective amino-sulfhydryl stapling on native peptides proteins. allow a fast of N-terminal cysteines (k2=1.54±0.18×103 M−1 s−1) under dilute aqueous conditions, enabling selectivity over other nucleophilic am...

Graphene quantum dots (GQDs) have been of high interest due to their size and optical characteristics, which improves when functional groups are added borders defects. In this work, the in vitro toxicity aqueous dispersion GQDs (w/wo amino-functionalization) was investigated two different cellular models (S. cerevisiae H9c2 cell line). Results yeast suggest that at up 25 % volume concentration,...