Chemoenzymatic synthesis of highly enantiomerically enriched secondary alcohols with a thiazolic core

Stereoselective preparative enzymatic acylation and hydrolysis/methanolysis of various C-substituted rac-thiazol-2-yl-methanols were achieved for the preparation of enantiopure or enantiomerically enriched, naturally occurring 2-hydroxymethylthiazoles. The absolute configurations of the resulting secondary alcohols were determined by a detailed ¹H NMR study of Mosher’s derivatives.     

Synthesis and optical nondestructive evaluation of GaN nanorods on silicon surfaces with gold catalyst

Nanometric gallium-nitride rods were grown on a silicon (1 1 1) substrate through a chemical vapor deposition process with gold particles as the catalyst. Randomly distributed gallium-nitride rods of 20–200 nm in diameter and of various densities and lengths were formed under different deposition conditions. Characterization analyses, such as scanning electron microscopy and optical reflection spectroscopy, have been carried out on samples containing gallium-nitride rods different in size, shape, length and density. While the scanning electron microscopy shows directly the images of the sample surfaces, the optical spectroscopy provides a nondestructive evaluation of the sample surfaces, especially helpful for checking the uniformity of the samples.     

Enantioselective analysis of venlafaxine and its active metabolites: A review on the separation methodologies

Venlafaxine (VFX) is a serotonin and norepinephrine reuptake inhibitor chiral drug used in therapy as an antidepressant in the form of a racemate consisting of R‐ and S‐VFX. The two enantiomers of VFX exhibit different pharmacological activities: R‐VFX inhibits both norepinephrine and serotonin synaptic reuptake, whereas S‐VFX inhibits only the serotonin one. R‐ and S‐VFX are metabolized in the liver to the respective R‐ and S‐O‐desmethylvenlafaxine (ODVFX), R‐ and S‐N‐desmethylvenlafaxine (NDVFX), and R‐ and S‐N,O‐didesmethylvenlafaxine (NODVFX). The pharmacological profile of ODVFX is close to that of VFX, whereas the other two chiral metabolites (NDVFX and NODVFX) have lower affinity for the receptor sites. The pharmacokinetics of the VFX enantiomers appear stereoselective, including the metabolism process. In the past 20 years, several studies describing the enantioselective analysis of R‐ and S‐VFX in pharmaceutical formulations and its chiral metabolites in biological matrices were published. These methods encompass liquid chromatography coupled with UV detection, mass spectrometry, or tandem mass spectrometry, and capillary electrophoresis. This paper reviews the published methods used for the determination of the individual enantiomers of VFX and its chiral metabolites in different matrices.     

High‐order implicit time integration for unsteady incompressible flows

The spatial discretization of unsteady incompressible Navier–Stokes equations is stated as a system of differential algebraic equations, corresponding to the conservation of momentum equation plus the constraint due to the incompressibility condition. Asymptotic stability of Runge–Kutta and Rosenbrock methods applied to the solution of the resulting index‐2 differential algebraic equations system is analyzed. A critical comparison of Rosenbrock, semi‐implicit, and fully implicit Runge–Kutta methods is performed in terms of order of convergence and stability. Numerical examples, considering a discontinuous Galerkin formulation with piecewise solenoidal approximation, demonstrate the applicability of the approaches and compare their performance with classical methods for incompressible flows. Copyright © 2011 John Wiley & Sons, Ltd.     

Associating divisors with quadratic differentials on Klein surfaces

We extend the notion and basic properties of quadratic differential divisors to a Klein surface, using the corresponding form’s divisors from the double cover of the Klein surface.     

Mild,Rapid, and Inexpensive Microwave-Assisted Synthesis of Allylic and Propargylic Esters

A variety of allylic and propargylic esters were rapidly prepared via microwave heating of their corresponding mixed anhydride derived from pivaloyl chloride. The reaction conditions were modified to account for the sterics of the alcohol and the electronics of the carboxylic acid.

Supplemental materials are available for this article. Go to the publisher's online edition of Synthetic Communications® to view the free supplemental file.     

Solvent-Free Microwave-Assisted Organic Reactions Preparation of β-Keto Esters

Microwave technique has been utilised in the preparation of β-keto esters. Two different procedures are described: transesterification of β-keto esters and ring opening of 2,2,6-trimethyl-1,3-dioxin-4-one.     

Synthesis and cytotoxicity evaluation of diastereoisomers and N-terminal analogues of tubulysin-U

Tubulysins are potent anti-mitotic natural compounds and a scalable and efficient synthetic route for generation of its analogues has been developed and extended to the synthesis of diastereoisomers and N-terminal analogues of tubulysin-U. Structure–activity-relationship studies on these synthetic analogues reaffirmed the significance of native stereochemistry of tubulysins for optimal biological activity and cytotoxicity. However, while modification of Tup stereochemistry has only minor effect on the tubulysins cytotoxicity, Tuv stereochemistry is critically important and modification of either Tuv stereocentre produced a dramatic drop in cytotoxicity.