Amodiaquine (AQ) is an antimalarial which is effective against chloroquino-resistant strains of Plasmodium falciparum but whose clinical use is severely restricted because of associated hepatotoxicity and agranulocytosis. "One-pot" synthesis of formamidines likely to be transformed into AQ derivatives is reported. Compared with AQ, the new compounds were devoid of in vitro cytotoxicity upon hum...

Pyrinodemin A 1, a cytotoxic marine alkaloid, was synthesized in a convergent and enantioselective fashion. The key steps are an asymmetric intramolecular dipolar cycloaddition of an oxazoline N-oxide to introduce the bicyclic ring system of the molecule, a cuprate coupling for the extension of the saturated chain and a B-alkyl Suzuki coupling for the introduction of a 3-pyridyl moiety. Reducti...

Here, we describe a simple and sensitive method that allows fluorescent detection of glycoproteins on polyvinylidene difluoride (PVDF) membrane. We used periodic acid oxidation of carbohydrate chains of glycoproteins and fluorescent labeling with 8-aminonaphthalene-1,3,6-trisulfonate (AN-TS) by reductive amination. We developed an additional method to enhance the ability of PVDF to absorb glyco...

Diazahexathia-24-crown-8 (2) has been isolated from the reaction mixture during the preparation of monoazatrithia-12-crown-4 (1). When N-Boc protected bis(2-chloroethyl)amine was employed as a starting material, N-Boc protected monoazatrithia-12-crown-4 (3) and N-Boc protected diazahexathia-24-crown-4 (4) were separated easily. Double-armed diazahexathia-24-crown-8 having two 3',5'-dichlorobenz...

Abstract N-Aryl-1,2,3,4-tetrahydroisoquinolines are obtained via a convenient and short protocol with broad range of substituents on both aromatic rings high functional group tolerance. Starting from readily available ortho-brominated aldehydes primary amines, condensation these building blocks under reductive conditions gives N-aryl 2-bromobenzylamines. The C-3/C-4-unit the tetrahydroisoquinol...

A nickel-catalyzed cross-coupling amination with weak nitrogen nucleophiles is described. Aryl halides as well aryl tosylates can be efficiently coupled a series of N-nucleophiles, including anilines, sulfonamides, sulfoximines, carbamates, and imines via concerted paired electrolysis. Notably, electron-deficient anilines sulfonamides are also suitable substrates. Interestingly, when benzopheno...

One-pot reaction of aldehydes or ketons with aniline derivatives was performed using NaBH4 and Fe3O4 magnetic nanoparticles (MNPs). The optimum amount of Fe3O4 MNPs was 5 mol% under solvent free condition. The corresponding products were obtained in good to excellent yields. The magnetically recoverable iron oxide nanoparticles are found to be efficient for synthesis of amine derivatives. These...