A practical and convergent synthesis of biologically active 1-(N-acyl)-1-aminoisoquinolines from the reaction of 2-alkynylbenzaldoximes with amides has been realized. The readily available amides could be activated with triflic anhydride (Tf2O) and could efficiently participate in the domino reaction of 2-alkynylbenzaldoximes when catalyzed by AgOTf, thus providing various acylated 1-aminoisoqu...

The synthesis of N-acetyl derivatives of α-amino acids (L–Gly, L–Val, L–Phe, L–Ile, L–Pro and L–Cys) using a simple and efficient method for preparation was carried out. The N-acetyl derivatives were obtained using acetic anhydride in basic conditions at room temperature. The methyl amides of N–acetyl amino acid were synthesized by mixed anhydride procedure using a Piv–Cl as a reagent. The conv...

The known procedures for the conversion of alkenylstannanes into the corresponding fluoroalkenes suffer from largely variable yields and a limited compatibility with functional groups; most notably, protodestannation becomes a serious issue whenever protic sites are present in the substrate. Outlined in this paper is a convenient alternative with a much improved application profile, which is la...

For the first time lactic acid was applied as an efficient and green catalyst for the one-pot three-component synthesis of amidoalkyl naphthols via the condensation between arylaldehydes, 2-naphthol and amides or urea under thermal solvent-free conditions in good to excellent yields. We have demonestrated a mild and efficient eco-friendly tandem synthesis of amidoalkyl naphthols using lactic ac...

The synthesis of various amides has been realised avoiding the use of any organic solvent from activation of carboxylic acids with CDI to isolation of the amides. Mechanochemistry was the key point of the process allowing rapid formation of the amide bond and efficient water-based purification of the final products.

An efficient strategy for the oxidative carbonylation of aromatic amides via C-H/N-H activation to form phthalimides using an Rh(III) catalyst has been developed. The reaction shows a preference for C-H bonds of electron-rich aromatic amides and tolerates a variety of functional groups.

Palladium dimers with sterically hindered phosphines have been shown to be excellent pre-catalysts for the aminocarbonylation of aryl halides to yield amides and one of them has been successfully employed as a pre-catalyst for the synthesis of (11)C-radiolabelled amides for PET imaging.

A catalyst based on a new biarylphosphine ligand (3) for the Pd-catalyzed cross-coupling reactions of amides and aryl chlorides is described. This system shows the highest turnover frequencies reported to date for these reactions, especially for aryl chloride substrates bearing an ortho substituent. An array of amides and aryl chlorides were successfully reacted in good to excellent yields.

A catalyst, based on a biarylphosphine ligand, for the Pd-catalyzed cross-coupling reactions of amides and aryl mesylates is described. This system allows an array of aryl and heteroaryl mesylates to be transformed into the corresponding N-aryl amides in moderate to excellent yields.