Observations on the Modified Wenker Synthesis of Aziridines and the Development of a Biphasic System

This document is the Accepted Manuscript version of a Published Work that appeared in final form in Journal of Organic Chemistry, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see http://dx.doi.org/10.1021/jo302615gA cheap and reliable process for the modified Wenker cyclization to afford aziridines has been achieved using biphasic conditions for a range of amino alcohol starting materials. A 100 mmol “one-pot” process has also been devised and enantiopurity of the starting amino alcohol is retained in the aziridine product

Synthesis and properties of some new 5-fluoro-6-(heterocyclyl) benzofuroxans

A series of 5-fluoro-6-(heterocyclyl) benzofuroxans (3b-e) have been prepared by hypochlorite oxidative cyclization of the respective 4-fluoro 5-(N-heterocyclyl)-2-nitroanilines (2b-e). The heterocyclyls include piprazine, N-(2-hydroxyethyl) piprazine, morpholine and thiomorpholine. Some bio-properties and spectral data these new derivatives are presented

مركبات حلقية من أكاسيد النيترايل (5)، 4-أمينو-1،2،4- أكساديازولين

nitrile, ketone and nitrogen.. Nitrile oxides undergo 1,3-dipolar cycloaddition with alkanone hydrazones to give 4-amino-1,2,4-oxadiazolines. Lead tetracetate oxidation of these compounds brings about smooth heteroring cracking into the correspondingتتفاعل أكاسيد النيترايل مع هيدرازونات الكيتونات معطية أمينوأوكساديازولين، أكسدة هذه المركبات باستعمال مركبات خلات الرصاص الرباعية أدت لتكسرها لمركبات النيترايل والكيتون والنيتروجين

New Synthesis and Antiparasitic Activity of Model 5-Aryl-1-methyl-4-nitroimidazoles

A number of 5-aryl-1-methyl-4-nitroimidazoles 5a-f have been synthesized in good yields by the Suzuki coupling reaction between 5-chloro-1-methyl-4-nitroimidazole (3) and arylboronic acids 4a-f, aided by dichlorobis-(triphenylphosphine)palladium(II), K2CO3, and tetrabutylammonium bromide in water at 70-80 °C. Compounds 5a-f were characterized by elemental analysis, NMR and MS spectral data. On the basis of in vitro screening data, 5-(3-chlorophenyl)-1-methyl-4-nitro-1H-imidazole (5f)exhibited potent lethal activity against Entamoeba histolytica and Giardia intestinalis with IC50 = 1.47 µM/mL, a value lower by a factor of two than that of the standard drug, metronidazole. The boosted activity of 5f was not accompanied by any increased cytotoxicity.The rest of the series also exhibited potent antiparasitic activity with IC50 valuesin the 1.72-4.43 µM/mL range. The cytotoxicity of the derivatives 5c and 5e was increased compared to the precursor compound, metronidazole, although they remain non-cytotoxic at concentrations much higher than the antiparasitic concentration of the two derivatives

Part VIII [1]. Convenient Synthesis and Antimicrobial Properties of Substituted Hexahydro[1,4]diazepino[2,3h]quinoline-9-carboxylic acid and Its Tetrahydroquino[7,8b]benzodiazepine Analog

molecule

Synthesis of Some Cyclic Methylene 1,3-Diaza Barbiturates Derivatives

The reaction of 1,3-dimethyl-5-bis(thioethyl)methylene barbituric acid (2) with various vic-diamines leads to the formation of the respective 1,3-diazamethylene barbiturate derivatives 3 (a-f) in high yields. Solid-state 13C-NMR, MS and IR spectral data were employed for the characterization of these compounds. Antimicrobial screening revealed that none of the newly synthesized compounds showed appreciable antibacterial activity