The preparation of a crystalline, peracetyl adamantanyl thiosialoside donor protected by an isothiocyanate group is described. On activation at -78 °C in the presence of typical carbohydrate acceptors, this donor gives high yields of the corresponding sialosides with exquisite α-selectivity. The high selectivity extends to the 4-O-benzyl-protected 3-OH acceptors, which are typically less reacti...

Chiral amines and amino acids play an important role in the pharmaceutical, agrochemical and chemical industry. They are frequently used as synthons for the preparation of various pharmaceutically active substances and agrochemicals, or as resolving agents for chiral acids. Consequently, there is a need for efficient methods to obtain the desired R or S enantiomer in an optically pure form. The...

A direct asymmetric hydrogenation of unprotected enamino esters and amides is described. Catalyzed by Rh complexes with Josiphos-type chiral ligands, this method gives beta-amino esters and amides in high yield and high ee (93-97% ee). No acyl protection/deprotection is required.

Antimicrobial natural preparations involving cinnamon, storax and propolis have been long used topically for treating infections. Cinnamic acids and related molecules are partly responsible for the therapeutic effects observed in these preparations. Most of the cinnamic acids, their esters, amides, aldehydes and alcohols, show significant growth inhibition against one or several bacterial and f...

The arylation of secondary acyclic amides has been achieved with diaryliodonium salts under mild and metal-free conditions. The methodology has a wide scope, allows synthesis of tertiary amides with highly congested aryl moieties, and avoids the regioselectivity problems observed in reactions with (diacetoxyiodo)benzene.

The heteroleptic calcium amides [{ArNC(Me)CHC(Me)NAr}Ca(NR(2))(THF)] (Ar=2,6-di-iso-propylphenyl, R=SiMe(3), Ph) and the homoleptic heavier alkaline earth amides, [M{N(SiMe(3))(2)}(2)] (M=Ca, Sr and Ba) are reported as pre-catalysts for the hydroamination of isocyanates.

The synthesis of aryl amides via the reactions of carboxylic acids and isocyanides in methanol was carried out in 78-95% yields under ultrasound irradiation. The method has wide applicability, and the protocol is mild, fast and efficient compared to the existing methods based on silent conditions.

A green and efficient one-pot three component reaction of 4-hydroxycoumarin or 1,3-dimethylbarbutyric acid, aryl glyoxals and amides (thioacetamide) has been developed in the presence of BF3- SiO2 nanoparticles in water. This method has several advantages such as high to excellent product yields in short reaction time, atom economy, environment friendly, reusable catalyst and no need for chroma...

Nano silica-H2SO4 is an efficient and mild catalysis system for the regeneration of aldehyde from aldoximes. Ketoximes are converted to amides by Beckmann rearrangement in the presence of nano silica-H2SO4. The reactions are carried out in solvent-free conditions under microwave irradiation (600 W) within 50-120 sec in good yields.