Macrocyclic compounds have potential to enable drug discovery for protein targets with extended, solventexposed binding sites. Crystallographic structures of peptides bound at such sites show strong surface complementarity and frequent aromatic side-chain contacts. In an effort to capture these features in stabilized small molecules, we describe a method to convert linear peptides into constrai...

Friedel-Crafts alkylation reaction of vinyltri-methoxysilane with styrene was performed in the pres-ence anhydrous AlCl3. Alkoxy(4-vinylphenethyl)silane has been obtained. The synthesized products were identified by 1H, 13C, COSY NMR, and FTIR spectroscopy. Calculations using quantum-chemical non-empirical density functional theory (DFT) method for between vinyltrimethoxysilane ortho-, meta- pa...

Isatin is a heterocyclic nitrogen compound that has attracted much interest in recent years due to its diverse biological and pharmacological activities. It can be used many medical applications, such as antidiabetic, antibiotic, anticancer agents. The isatin molecule also prepared from different substrates by various methods, the methods of Sandmeyer, Stolle, Gassman, Meanwell Hewawasam others...

The first immobilization of a MacMillan's first generation organocatalyst onto dendritic support is described. A modified tyrosine-based imidazolidin-4-one was grafted to a soluble high-loading hyperbranched polyglycerol via a copper-catalyzed alkyne-azide cycloaddition (CuAAC) reaction and readily purified by dialysis. The efficiency of differently functionalized multivalent organocatalysts 4a...

A novel triphenylphosphine-based porous polymer (TPDB) with a high Brunauer-Emmett-Teller (BET) surface area was synthesized through Friedel-Crafts alkylation of triphenylphosphine and α-dibromo-p-xylene. Then, the functional hydroxyl groups were successfully grafted onto the polymer framework by post modification of TPDB with 3-bromo-1-propanol (BP) and triethanolamine (TEA). The resulting sam...

A new material MIT-1 comprised of delaminated MWW zeolite nanosheets is synthesized in one-pot using a rationally designed organic structure-directing agent (OSDA). The OSDA is comprised of a hydrophilic head segment that resembles the OSDA used to synthesize the zeolite precursor MCM22(P), a hydrophobic tail segment that resembles the swelling agent used to swell MCM22(P), and a di-quaternary ...

Computational calculations based on experimental results shed light on the mechanistic proposal for a Friedel-Crafts alkylation reaction between indole and nitroalkenes, catalysed by a chiral aminoindanol-derived thiourea. In our hypothesis both substrates are simultaneously coordinated to the catalyst in a bifunctional mode. This study elucidates the crucial role played by the hydroxyl group o...

The 1,2-aminoindanol scaffold has been found to be very efficient, enhancing the enantioselectivity when present in organocatalysts. This may be explained by its ability to induce a bifunctional activation of the substrates involved in the reaction. Thus, it is easy to find hydrogen-bonding organocatalysts ((thio)ureas, squaramides, quinolinium thioamide, etc.) in the literature containing this...

ammonium monovanadate (nh4vo3) has been devoted as an efficient, commercially available, eco-friendly and reusable catalyst for the synthesis of bis(indolyl)methanes (bims), oxindole derivatives and also michael adducts of indoles at 50 °c under solvent-free conditions. the reusability of this solid acid catalyst in addition with its selectivity has also been examined.