Diastereoselective aldol reaction of N,N-dibenzyl-alpha-amino aldehydes with ketones catalyzed by proline

[reaction: see text] L-proline-catalyzed direct aldol reaction of L-amino acid-derived N,N-dibenzyl amino aldehydes with acetone, cyclopentanone, or hydroxyacetone provides gamma-amino-beta-hydroxy- or gamma-amino-alpha,beta-dihydroxy-ketones with moderate to excellent yields and diastereoselectivities.     

The best constant of the Moser-Trudinger inequality on

We consider the best constant of the Moser-Trudinger inequality on under a certain orthogonality condition. Applying Moser's calculation, we construct a counterexample to the sharper inequality with the condition.

     

Synthesis of a new class of furan-fused tetracyclic compounds using o-quinodimethane chemistry and investigation of their antiviral Activity

The synthesis and evaluation of antiviral activity of new furan-fused tetracyclic compounds are described. The syntheses were satisfactorily achieved on the basis of o-quinodimethane chemistry, using furan-containing benzocyclobutene derivatives as a substrate, in high generality and stereoselectivity. The various derivatives thus synthesized were examined on their inhibitory activity on virus growth using a hemagglutinin (HA) method, leading to a discovery of promising candidates for new antiviral drugs having high activity and good therapeutic index.     

Development of a method for evaluating drug-likeness and ease of synthesis using a data set in which compounds are assigned scores based on chemists' intuition

The concept of drug-likeness, an important characteristic for any compound in a screening library, is nevertheless difficult to pin down. Based on our belief that this concept is implicit within the collective experience of working chemists, we devised a data set to capture an intuitive human understanding of both this characteristic and ease of synthesis, a second key characteristic. Five chemists assigned a pair of scores to each of 3980 diverse compounds, with the component scores of each pair corresponding to drug-likeness and ease of synthesis, respectively. Using this data set, we devised binary classifiers with an artificial neural network and a support vector machine. These models were found to efficiently eliminate compounds that are not drug-like and/or hard-to-synthesize derivatives, demonstrating the suitability of these models for use as compound acquisition filters.     

A counterexample to Sorenson’s conjecture: The finitely generated case

It is shown that there exists a finitely generated, left amenable semigroup which is right cancellative but not left cancellative. This resolves negatively a question raised by M. Klawe.     

Asymptotic behavior of certain delay differential equations with forcing term

We study the asymptotic behavior of solutions of the following forced delay differential equation:

Some sufficient conditions that guarantee every solution of the equation to converge to zero are obtained. The results obtained are applied to some well-known delay differential ecological equations with forcing term.     

Alignment-free optical modules using solder-bump-bonding technique for free-space optical interconnections

We propose alignment-free optical modules using a solder-bump-bonding technique for constructing free-space optical interconnection systems without a special alignment procedure. Bonding pads for mounting an optoelectronic device chip are fabricated by exposing a photosensitive resin film to light traveling through the optical system of the module so that the image positions of the bonding pads on both image planes of the optical interconnection system are aligned with each other. A device chip is mounted by solder-bump bonding and is set at a proper position by the surface tension of molten solder. The effectiveness of the technique is verified by constructing alignment-free optical modules.     

Facile synthesis of aryl ether dendrimer from unprotected AB2 building blocks using thionyl chloride as an activating agent

[structure: see text] A novel, rapid, inexpensive, and highly efficient convergent approach for the synthesis of a Fréchet- type aryl ether dendrimer using thionyl chloride has been developed. In this method, the purification of each dendron and a dendrimer occurs by recrystallization, extraction, and precipitation. The MALDI-TOF MS spectrum supported the formation of the G2, G3, and G4 dendrons and the star-shaped G4 dendrimer.     

A new triterpene synthase from Arabidopsis thaliana produces a tricyclic triterpene with two hydroxyl groups

[structure: see text] Thirteen oxidosqualene cyclase homologues exist in the genome of Arabidopsis thaliana. One of these genes, At4g15340, was amplified by PCR and expressed in yeast. The yeast transformant accumulated tricyclic triterpene, (3S,13R)-malabarica-17,21-dien-3,14-diol (arabidiol), whose structure was determined by NMR and MS analyses. Its epoxide analogue, (3S,13R,21S)-malabarica-17-en-20,21-epoxy-3,14-diol (arabidiol 20,21-epoxide), was also isolated from the transformed yeast. This is the first example of a triterpene synthase that yields a tricyclic triterpene with two hydroxyl groups.     

Biomolecular embossing

The replica molding and embossing of DNA texture has been achieved using a conventional polyurethane mold. The final process requires no additional or separate extraction phases. The polyurethane replica is stable up to 150 degrees C and possesses a good longevity and a capacity to emboss a biological entity into a thermosetting plastic such as poly(ethylene terephthalate).