Letters in Organic Chemistry - Volume 15, Issue 6, 2018

Background: Up to date, numerous attempts for the synthesis of potentially interesting medicinally important heterocyles and organic compounds by application of a wide range of homogeneous and heterogeneous catalysts under green conditions have been made and published. The abundance and variety of diseases and the needs of mankind for treatment of them have made these attempts inevitable. Furthermore, Read More

Background: Phorboxazole is a polycyclic natural product which exhibits antitumor activity. The synthesis of C20-C26 segment of phorboxazoles, possessing 5 contiguous stereocenters, is described. Methods: A double diastereoselective aldol reaction using an Evans chiral oxazolidinone with a chiral aldehyde generates the C23-C25 stereocenters. Chain extension via Horner-Wadsworth-Emmons olefination and subsequent funct Read More

Fluorescence and photoisomerization studies on donor-acceptor substituted phenyl conjugated molecules [e.g. 2-[(1E)-2-(4-nitrophenyl)ethenyl]furan (trans-1) and 2-[(1E)-2-(4-aminophenyl)- ethenyl]furan (trans-2)] in solvents of varying polarity suggest that ethenylfuran trans-1, with strong electron acceptor, exhibits large solvatochromic red shifted fluorescence maximum, highly dipolar excited state, an Read More

Classical methods for the synthesis of diarylmethylpiperazine drugs generally lead to the generation of high levels of waste. In this study, we have developed a simple and efficient route to the anti-histamine drugs Meclizine 1, Buclizine 2, Clocinizine 3, Cinnarizine 4, Flunarizine 5 and Flotrenizine 6. The advantage of this route lies on the replacement of harmful alkyl halides by readily available alcohols to achieve the N-alkylation of Read More

Background: Blockade of kainate receptors is an emerging strategy to treat neurodegenerative diseases, including Parkinson's disease as well as to treat epilepsy. In particular, non-competitive antagonists of kainate receptors are promising due to the expected good safety profile. We present here synthesis, experimental and computational studies of N-(4-amino-6-oxo-1,6-dihydropyrimidin-5- yl)benzamide which is an intermed Read More

A green and efficient approach to aryl azides, in very short reaction times and excellent yields, has been developed via the reaction of arylboronic acids with sodium azide under CuI catalysis in neat Water Extract of Banana (WEB). The entire process provided compensations over conventional heating in that reactivity of the less reactive arylboronic acids was induced as well as the reaction time was reduced. We have described Read More

Background: Esters of fatty acids with alcohols especially polyols (polyhydroxy alcohols) have found considerable applications as synthetic greases, synthetic lubricants, in cosmetics, food, and paint industries. Industrial or conventional esterification is carried out by the condensation of carboxylic acids with alcohols in the presence of an acid catalyst of homogenous nature. The development of heterogeneous / solid acid catalysts o Read More

The importance and wide application of hydrazones are due to a broad spectrum of biological activities that they possess. The biological activity generally depends on the pH values of the media which have influence on the extent of ionization of organic compounds. The dissociation process of five 4-methoxybenzaldehyde benzoylhydrazones in aqueous sodium hydroxide media was determined using UV spectroscopy method Read More

An efficient synthesis of 2,3-dihydroquinazolin-4(1H)-one derivatives using nanocrystalline magnesium oxide (nano-MgO) as a catalyst from 2-aminobenzamide and various aldehydes/ketones under aqueous conditions at room temperature is described. Nano-MgO was synthesized by the precipitation and hydrothermal treatment of aqueous salt solution as reported previously. The structure of nano-MgO was characterized Read More

2,4,5-Triaryl-1H-imidazoles were synthesized from benzyl bromides under Kornblum oxidative condition. The reaction proceeded via an in situ oxidation followed by condensation to afford the desired products in good yields.

Background: Aldehydes were converted to carboxylic acids using sodium hypochlorite as oxidant in a single step, involving microwave assistance and without a metal catalyst in basic media. The use of microwave irradiation increased both conversion and yield due to an easier work-up and the reaction time was reduced. Two advantages of this oxidation are the relatively low cost and low pollution. This oxidative method has Read More

In the present study, a new class of triazino-caffeine derivatives with good antimicrobial activities is reported. Eight new triazino-caffeine derivatives were synthesized via Mitsunobu reaction, followed by intramolecular cyclization. Their chemical structures were established on the basis of elemental analysis, IR, 1H NMR, mass spectral data as well as through an alternate synthetic route. The compounds were also screened Read More

Background: Over the last few years, one of the primary focuses of our research group has been the synthesis and biological evaluation CANs featuring structural and/or configurationally alterations on the carbocyclic moiety. We previously reported an enlarged group of diversely functionalized amino cyclopentenols, cyclopentenols and cyclopentenones as useful precursors in the synthesis and posterior biological Read More