Current Organic Synthesis - Volume 13, Issue 4, 2016

In the armamentarium of antifungal agents, appropriately functionalized triazines and their derivatives have received considerable attention in the recent past. In this focus review, we have highlighted the investigations regarding antifungal activities of triazines and their derivatives.

The continuous study on the preparation of different types of carboranylphosphine ligands and their derivatives is of great interest because of their rich coordination chemistry and promising applications in a variety of important fields. The diverse reactivities and particular bonding modes of novel transition metal complexes containing carboranylphosphine-based ligands have attracted extensive attention. Herein, we describe Read More

Trifluoromethylated amines, especially optically active ones, are very important synthetic building blocks in the design of bioactive products. Over the past decades, the development of highly efficient methods for asymmetric synthesis of Trifluoromethylated amines and their derivatives has attracted a continuing interest. A brief overview will give an insight into the asymmetric synthesis of trifluoromethylated amines and thei Read More

Glycosylated nitrogen-containing heterocyclic compounds which hold wide range of anticancer activities are drawing much attention from researchers Many efforts have been made for developing more novel and efficient ways to synthesize these compounds. The purpose of this review is to sum up recent advances in the synthesis of glycosylated nitrogen-containing heterocyclic compounds and their potential anticancer activities.

Mycobacterium tuberculosis is the causative agent of tuberculosis (TB), which has been and still remains a serious disease to the global human population causing millions of deaths worldwide. The recent increase in the number of multi-drug resistant clinical isolates of M. tuberculosis has created an urgent need for the discovery and development of new antituberculosis drugs. The recent researches focusing on natural pr Read More

In this review, we tried to highlight the recent advances in the Biginelli reaction, leading to the synthesis of 3,4-dihydropyrimidin-2(1H)-ones, albeit only those conducted under microwave irradiation. The merits and drawbacks of these reactions are compared and discussed with those performed under conventional heating. Dedicated to kazem Kargosha, in the occasion of his honorable retirement as a Professor in Ana Read More

An efficient and convenient route for synthesis of novel bis 4H-chromene-3- carbonitrile derivatives is reported. The synthetic pathway involves one pot, multi-component reaction of bis-aldehydes, malononitrile, and dimedone in the presence of a catalytic amount of piperidine. A stepwise approach for the synthesis of the target compounds was also investigated.

4,9-Dihydro-3H-β-carboline and 6-methoxy-4,9-dihydro-3H-β-carboline were subjected to catalyst-free one-pot α-arylation with 1- or 2-naphthol, 6-hydroxyquinoline or 5-hydroxyisoquinoline as N-containing analogues via direct aza-Friedel-Crafts reactions. The procedure was then extended to other electron-rich aromatic compounds, such as indole or indole-2-carboxylic acid, to yield new indole γ-amino acid derivatives containi Read More

The triphenylmethyl group can be used as a steric buttress to drive otherwise unfavorable intramolecular Diels-Alder cycloaddition reactions. Using this strategy, we attempted to synthesize the cycloadducts 9-triphenylmethylaza-1,4-oxidobicyclo[4.4.0]dec-2-ene (3b) and 10-triphenylmethylaza-1,4-oxidobicyclo[5.4.0]undec-2-ene (3c) from furfurylamine-based starting materials, and it was found that the presence of the buttress Read More

A general and simple procedure for the synthesis of 3-nitroformazan using arenediazonium tosylates was developed. This convenient procedure can be applied for the preparation of 3-nitroformazans containing electron-donating or electron-withdrawing groups. First the anomaly 1,5-bis(4-methoxyphenyl)-3-nitroformazan was synthesized as the mixture of TSSC (trans-syn, s-cis) and previously unknown for 3-nitroformazans Read More

Potassium 4-iodylbenzenesulfonate (PIBS) is a thermally stable and water soluble hypervalent iodine oxidant particularly useful as a recyclable reagent for oxidative iodination of alkenes, alkynes and ketones. This reagent can be effectively recovered from the reaction mixture by treatment of the aqueous layer with Oxone at 60 °C followed by filtration of the precipitate.

Ethyl octyl phosphite (EOP), a dialkyl phosphite with mixed alkyl groups was prepared, and utilized in the Kabachnik–Fields reaction. The condensation of EOP, paraformaldehyde and primary or secondary amines used in equimolar quantities afforded new α-aminophosphonates under microwave conditions. Methylation of the -α(alkylamino)phosphonates was also investigated. The double phospha-Mannich reaction of p Read More

Anthracene based amino acids are synthesized as a new class of fluorescence sensors for the detection of metal ions. Synthesized amino acids were characterized with 1H NMR, 13C NMR, IR and LCMS spectroscopy. The electro- and photo-luminescent spectra of the fluorescent amino acids were studied and the interaction of 18b with metal ions was discussed. Among various metal ions screened, the fluorescence of the ami Read More

A catalyst-free condensation reaction of α,β-unsaturated ketones and sodium sulfide in CH3CN-H2O mixture (1:1) was established to prepare a variety of polysubstituted tetrahydrothiopyrans in good to excellent yields. The obtained tetrahydrothiopyrans were oxidized with MCPBA to the corresponding sulfoxides in good yields. The present research is the first report on synthesis of polysubstituted tetrahydrothiopyran sulfoxides