Letters in Organic Chemistry - Volume 20, Issue 8, 2023

An efficient and environmentally-friendly protocol for the synthesis of 2- (arylamino) thiazoles has been investigated. The two-step, three-component reaction of aryl ketones, Nbromosuccinimide, and thiourea derivatives was performed using [bmim][BF4] ionic liquid as a solvent in one pot and gave products in good to excellent yields. Furthermore, the ionic liquid could be reused up to the 5th time without a considerabl Read More

[Hydroxy(tosyloxy)iodo]benzene mediated the oxidative cleavage of pyridyl hydrazones to regenerate aryl ketones efficiently. Reaction occurred by simply stirring the hydrazone with hypervalent iodine reagent in dichloromethane at room temperature, where aryl ketones are produced up to 90% yield.

A convenient, efficient method for synthesising indole-3-substituted-2-benzimidazoles and benzothiazoles was carried out using N-arylation followed by condensation-oxidation protocol. Narylation of 1H-indole-3-carbaldehyde was carried out via CuI/DMED to yield 1-(3-((tertbutylsulfonyl) methyl)phenyl)-1H-indole-3-carbaldehyde. Condensation using various o-phenylenediamines in the presence of CAN/DMF as oxidant furn Read More

An important bioactive heterocycle having several uses in medicinal chemistry, synthetic organic chemistry, material chemistry, and natural product is indole along with its analogues. Many bioactive indole-based heterocycles have important antibacterial, anti-inflammatory, analgesic, antiviral, antimalarial, chemotherapeutic, antifungal, and anti-TB effects, as well as antioxidant capabilities. Several well-known medicati Read More

Indole is an important heterocyclic molecule having a number of pharmacologically useful properties. Adolf von Baeyer synthesized indole by reducing oxindole in the presence of a catalytic amount of zinc dust in 1866. A number of studies have been conducted and many more are in the pipeline to investigate the medicinal potential of indole and its derivatives. Indomethacin, Indolmycin, Oxypertine, Yohimbine, Pindolol, a Read More

Firstly, 2-amino aromatic ketones were synthesized by o-acylation of p-substituted anilines with nitrile under Sugasawa conditions, and the yield was up to 90.1%. Then, 4-pyridinylquinoline derivatives were synthesized by Friedlander reaction with α-methylene ketones, and the yield was up to 81.9%. The structures of five 2-amino aromatic ketones and eighteen substituted quinolines were characterized by MS, 1H NMR, and 13 Read More

A three-component reaction under ultrasound irradiation and with a catalytic amount of citric acid was presented for the synthesis of a series of 2-aryl-quinazolin-4(1H)-ones with excellent efficiency and short reaction time. This one-pot reaction with 2-aminobenzonitrile, ammonium hydroxide or glycine and benzaldehydes is a clean and safe route for the environment at room temperature. Mild reaction conditions, green enviro Read More

A coordination polymer Zr-CIA was developed and employed as a stable and effective catalyst for the alkylation of amines with alcohols or benzyl amines. The Zr-CIA as a new coordination polymer was prepared from 1-(carboxymethyl)-1H-indole-3-carboxylic acid and ZrCl4 through a simple and effective solvothermal method and characterized by scanning electron microscopy (SEM), transmission electron microscopy (TEM), Read More