A new safety-catch protecting group and linker for solid-phase synthesis

The use of two derivatives of 2-methoxy-4-methylsulfinylbenzyl alcohol is demonstrated as a safety-catch protecting group and linker for solid-phase peptide synthesis. The protecting group and linker are stable to TFA and are readily removed under reductive acidolytic conditions.     

18‐Crown‐6 Catalyzed Microwave‐mediated Synthesis of Symmetric Bis‐Heterocyclic Compounds under Solvent‐free Condition

An efficient, solvent‐free and 18‐crown‐6 catalyzed method for the synthesis of N‐alkyl‐4‐(4‐(5‐(2‐(alkyl‐amino)thiazol‐4‐yl)pyridin‐3‐yl)phenyl)thiazol‐2‐amine, N‐alkyl‐4‐(5‐(2‐alkyamino)thiazol‐4‐yl)pyridine‐3‐yl)thiazol‐2‐amine, and 4,4′‐bis‐{2‐[amino]‐4‐thiazolyl}biphenyl bis‐heterocyclic derivatives via microwave accelerated cyclization is presented.     

Numerical Simulation of Delft-Jet-in-Hot-Coflow (DJHC) Flames Using the Eddy Dissipation Concept Model for Turbulence–Chemistry Interaction

In this paper, we report results of a numerical investigation of turbulent natural gas combustion for a jet in a coflow of lean combustion products in the Delft-Jet-in-Hot-Coflow (DJHC) burner which emulates MILD (Moderate and Intense Low Oxygen Dilution) combustion behavior. The focus is on assessing the performance of the Eddy Dissipation Concept (EDC) model in combination with two-equation turbulence models and chemical kinetic schemes for about 20 species (Correa mechanism and DRM19 mechanism) by comparing predictions with experimental measurements. We study two different flame conditions corresponding to two different oxygen levels (7.6% and 10.9% by mass) in the hot coflow, and for two jet Reynolds number (Re = 4,100 and Re = 8,800). The mean velocity and turbulent kinetic energy predicted by different turbulence models are in good agreement with data without exhibiting large differences among the model predictions. The realizable k-ε model exhibits better performance in the prediction of entrainment. The EDC combustion model predicts too early ignition leading to a peak in the radial mean temperature profile at too low axial distance. However the model correctly predicts the experimentally observed decreasing trend of lift-off height with jet Reynolds number. A detailed analysis of the mean reaction rate of the EDC model is made and as possible cause for the deviations between model predictions and experiments a low turbulent Reynolds number effect is identified. Using modified EDC model constants prediction of too early ignition can be avoided. The results are weakly sensitive to the sub-model for laminar viscosity and laminar diffusion fluxes.     

Two dimensional electrophoretic analysis of human tears: collection method in dry eye syndrome

Tear proteomics, by 2-DE, can give a fingerprint of the protein profile, which is well suited in clinical proteomics for biomarker identification and in diagnostics. The mode of tear collection can influence the representation of the proteins in the tear and therefore it is important to use the appropriate method. In this study, capillary and Schirmer mode of tear collection was done in the healthy controls and the Schirmer method was validated in dry eye syndrome conditions. 2-D PAGE of normal and dry eye tear was performed using pH 3-10 linear IPG strips followed by 13% SDS-PAGE. The spot intensity was analyzed by the PD quest software. The two methods were compared using Bland-Altman statistical tool. The 2-D map of capillary and Schirmer tear showed 147 ± 8 spots and 145 ± 7 spots respectively. Both the collection methods were in agreement with each other and were comparable. Dry eye tear protein showed differential expression of proteins as observed in 25-35 kDa region. One of the significantly reduced protein was identified as proline-rich 4 protein. Schirmer method of tear collection is reliable in patients with dry eye, which can display the differential protein expression and help in biomarker identification.     

Stoichiometry-controlled cycloaddition of azomethine ylide with dipolarophiles: chemoselective and regioselective synthesis of bis- and tris-spirooxindole derivatives

A new series of bis- and tris-spirooxindole derivatives have been synthesized by controlling the molar equivalent of in situ generated azomethine ylides in [3+2]-cycloaddition reactions with dipolarophiles. The structural elucidation on the basis of IR, ¹H NMR, ¹³C NMR, and mass spectral data of these compounds established the highly chemoselective and regioselective formation of spirooxindole derivatives. Single crystal X-ray analysis of compound 4g and 2D NMR analysis of compound 5a confirmed the structures of bis- and tris-spirooxindole derivatives.     

Facile synthesis of novel dispiroheterocylic derivatives through cycloaddition of azomethine ylides with acenaphthenone-2-ylidine ketones

The regioselective synthesis of a series of novel dispiropyrrolidines and dispiropyrrolizidines has been accomplished through intermolecular 1,3-dipolar cycloaddition of azomethine ylides obtained from 1,2-diones like isatin and acenaphthenequinone with acenaphthenone-2-ylidine ketone dipolarophiles in methanol under reflux conditions.     

Incorporation of triazole into a quinoline-rhodamine conjugate imparts iron(iii) selective complexation permitting detection at nanomolar levels

Two new rhodamine based probes 1 and 2 for the detection of Fe(3+) were synthesized and their selectivity towards Fe(3+) ions in the presence of other competitive metal ions tested. The probe 1 formed a coloured complex with Fe(3+) as well as Cu(2+) ions and revealed the lack of adequate number of coordination sites for selective complexation with Fe(3+). Incorporation of a triazole unit to the chelating moiety of 1 resulted in the probe 2, that displayed Fe(3+) selective complex formation even in the presence of other competitive metal ions like Li(+), Na(+), K(+), Cu(2+), Mg(2+), Ca(2+), Sr(2+), Cr(3+), Mn(2+), Fe(2+), Co(2+), Ni(2+), Zn(2+), Cd(2+), Hg(2+) and Pb(2+). The observed limit of detection of Fe(3+) ions (5 × 10(-8) M) confirmed the very high sensitivity of 2. The excellent stability of 2 in physiological pH conditions, non-interference of amino acids, blood serum and bovine serum albumin (BSA) in the detection process, and the remarkable selectivity for Fe(3+) ions permitted the use of 2 in the imaging of live fibroblast cells treated with Fe(3+) ions.