Stereoselective synthesis of polyhydroxylated aminocyclohexanes

The stereoselective synthesis of a series of di- and tri-hydroxylated aminocyclohexane derivatives has been developed. A one-pot, two step tandem process involving an Overman rearrangement and a ring closing metathesis reaction has been utilised for the asymmetric synthesis of (1S)-1-(2',2',2'-trichloromethylcarbonylamino)cyclohexa-2-ene. Oxidation of this cyclohexene derivative was then studied leading to the preparation of two diol analogues in excellent stereoselectivity. (1S)-1-(2',2',2'-trichloromethylcarbonylamino)cyclohexa-2-ene was then converted to a novel allylic alcohol via a 4,5-dihydro-1,3-oxazole. Functionalisation of this allylic alcohol by Upjohn dihydroxylation conditions or by a directed epoxidation/hydrolysis sequence of reactions allowed the synthesis of two dihydroconduramines in excellent stereoselectivity. The stereochemical assignment of all compounds prepared was confirmed by NOE experiments or X-ray structure determination.     

Herbicidal activity of culture filtrates of Trichoderma spp. against two problematic weeds of wheat

The herbicidal potential of culture filtrates of four Trichoderma spp., namely Trichoderma harzianum Rifai, Trichoderma pseudokoningii Rifai, Trichoderma reesei Simmons and Trichoderma viride Pers., was evaluated against two problematic weeds of wheat, Phalaris minor L. and Rumex dentatus L. In laboratory bioassays, generally, metabolites of all four Trichoderma species significantly reduced various root and shoot growth parameters of the two target weed species. The original concentrations of the culture filtrates of all Trichoderma spp., except T. harzianum, significantly reduced various parameters of root and shoot growth of wheat seedlings. In a foliar spray bioassay, the culture filtrates of all four Trichoderma spp. significantly diminished root and shoot biomass of R. dentatus. The effect of these filtrates on the shoot growth of P. minor and wheat was not significant. Culture filtrates of the four Trichoderma species were successively extracted with butanol, n-hexane, chloroform and ethyl acetate. In detached leaf injection bioassays, n-hexane fractions (3 mg mL(-1)) of T. pseudokoningii, T. reesei and T. viride, and ethyl acetate fractions of T. horzianum and T. pseudokoningii were found to be toxic against R. dentatus. This study concludes that the culture filtrates of Trichoderma species have herbicidal potential in the control of R. dentatus.     

Antioxidant activity of some lichen metabolites

Antioxidant activity of several classes of lichen metabolites were assessed in the in vitro superoxide radical (SOR), nitric oxide radical and 2,2-diphenyl-1-picrylhydrazil radical scavenging assays. The despsides sekikaic acid and lecanoric acid showed promising antioxidant activity in SOR assay with IC?? values of 82.0?±?0.3?μmol and 91.5?±?2.1?μmol, respectively, while the depsidone lobaric acid exhibited an IC?? value of 97.9?±?1.6?μmol, all relative to the standard, propyl gallate (IC???=?106.0?±?1.7?μmol). One of the most abundant mononuclear phenolic compounds, methyl-β-orcinol carboxylate was found to be a potent NO scavenger (IC???=?84.7?± 0.1?μmol), compared to the standard rutin (IC???=?86.8?±?1.9?μmol).     

Effect of inclusion complex on nitrous acid reaction with flavonoids

The kinetic of the nitrous acid reactions with quercetin and catechin has been studied using spectrophotometric method in aqueous solution. The results show that these antioxidants participate in oxidation reactions with nitrous acid which is derived from protonation of nitrite ion in mild acidic conditions. Corresponding o-quinones as relatively stable products were detected by spectrophotometric techniques. pH dependence of the reactions has been examined and the rate constants of reactions were obtained by non-linear fitting of kinetic profiles. The effect of β-cyclodextrin on the oxidation pathway was another object of this study. It is shown that β-cyclodextrin has an inhibitory effect on the oxidation reaction. The rate constants of oxidation reactions for complexed forms and their stability constants were obtained based on changes in the reaction rates as a function of β-cyclodextrin concentration.     

Entirely green protocol for the synthesis of β-aminoketones using saccharose as a homogenous catalyst

Saccharose was applied as an efficient and homogenous catalyst for a one-pot, three-component Mannich reaction for the formation of β-aminoketones from aromatic aldehydes, anilines, and acetophenone at ambient temperature in excellent yields. This protocol has the following advantages: mild conditions, high yields, clean reaction profiles, operational simplicity, and environmentally benign and simple work-up procedures.     

Recent trends in the synthesis of 1,2,3-thiadiazoles

Abstract

1,2,3-Thiadiazoles, structurally active pharmacophores have attracted significant attention of synthetic chemists, medicinal and pharmaceutical researchers because of their versatile biological activities against various diseases such as herbicidal, insecticidal, antiviral, antitumor, antimicrobial, anticancer, plants activator and anti-amoebic activities. A literature survey of the last decade presented in this review article summarizes the major synthetic approaches, methodologies and strategies adopted for the synthesis of 1,2,3-thiadiazole scaffolds which will be help for medicinal chemists and pharmacists in future synthesis and development of novel therapeutic agents.     

Nonclassical Lie symmetry and conservation laws of the nonlinear time-fractional Korteweg–de Vries equation

In this paper, we use the symmetry of the Lie group analysis as one of the powerful tools that deals with the wide class of fractional order differential equations in the Riemann–Liouville concept. In this study, first, we employ the classical and nonclassical Lie symmetries(LS) to acquire similarity reductions of the nonlinear fractional far field Korteweg–de Vries(KdV)equation, and second, we find the related exact solutions for the derived generators. Finally,according to the LS generators acquired, we construct conservation laws for related classical and nonclassical vector fields of the fractional far field Kd V equation.     

A New Two-Stage Algorithm for Solving Optimization Problems

Optimization seeks to find inputs for an objective function that result in a maximum or minimum. Optimization methods are divided into exact and approximate (algorithms). Several optimization algorithms imitate natural phenomena, laws of physics, and behavior of living organisms. Optimization based on algorithms is the challenge that underlies machine learning, from logistic regression to training neural networks for artificial intelligence. In this paper, a new algorithm called two-stage optimization (TSO) is proposed. The TSO algorithm updates population members in two steps at each iteration. For this purpose, a group of good population members is selected and then two members of this group are randomly used to update the position of each of them. This update is based on the first selected good member at the first stage, and on the second selected good member at the second stage. We describe the stages of the TSO algorithm and model them mathematically. Performance of the TSO algorithm is evaluated for twenty-three standard objective functions. In order to compare the optimization results of the TSO algorithm, eight other competing algorithms are considered, including genetic, gravitational search, grey wolf, marine predators, particle swarm, teaching-learning-based, tunicate swarm, and whale approaches. The numerical results show that the new algorithm is superior and more competitive in solving optimization problems when compared with other algorithms.     

Synthesis of guanidinium‐based anion exchange membranes and their stability assessment

Alkaline fuel cells potentially offer improved conversion efficiency and the prospect of using non‐noble metal catalysts; however, low conductivity and fast degradation of anion exchange membranes (AEMs) prevent their widespread application. In this work, a series of novel composite AEMs were synthesized by incorporating guanidinium‐based polymers into a porous polytetrafluoroethylene (PTFE) film. The guanidinium‐based polymers were polymerized using a condensation process between a guanidinium salt and two different diamines so that the guanidinium cations were tethered to the polymer backbone to enhance both conductivity and durability. In addition, polymer crosslinking was conducted to further reinforce the mechanical strength of the membranes and interlock the guanidinium moieties to the porous PTFE. It was found that the ionic conductivity of the synthesized membrane reached up to approximately 80 mS cm^?1 at 20°C in deionized water. These membranes also exhibited superior stability compared to commercial quaternary ammonium AEMs after being exposed in 5 M KOH solution at 55°C for 50 h. Copyright © 2013 John Wiley & Sons, Ltd.