Scalable Synthesis of TRPV1 Antagonist Bipyridinyl Benzimidazole Derivative via the Suzuki-Miyaura Reaction and Selective SeO Oxidation.

In this study, a kilogram-scale synthesis of a potent TRPV1 antagonist, is described. To synthesize bipyridinyl benzimidazole derivative , we have developed a scalable Suzuki-Miyaura reaction capable of providing a key intermediate, 6'-methyl-3-(trifluoromethyl)-2,3'-bipyridine , on a kilogram scale. Then, unlike the existing oxidation reaction pathway, two synthetic routes that can be applied to mass production of bipyridinyl carboxylic acid intermediate or aldehyde intermediate were developed by appropriately controlling the oxidation reaction using a selenium dioxide oxidizing agent.

Discovery of an Orally Bioavailable Benzofuran Analogue That Serves as a β-Amyloid Aggregation Inhibitor for the Potential Treatment of Alzheimer's Disease.

We developed an orally active and blood-brain-barrier-permeable benzofuran analogue (8, MDR-1339) with potent antiaggregation activity. Compound 8 restored cellular viability from Aβ-induced cytotoxicity but also improved the learning and memory function of AD model mice by reducing the Aβ aggregates in the brains. Given the high bioavailability and brain permeability demonstrated in our pharmacokinetic studies, 8 will provide a novel scaffold for an Aβ-aggregation inhibitor that may offer an alternative treatment for AD.

Broadband infrared photoluminescence in silicon nanowires with high density stacking faults.

Making silicon an efficient light-emitting material is an important goal of silicon photonics. Here we report the observation of broadband sub-bandgap photoluminescence in silicon nanowires with a high density of stacking faults. The photoluminescence becomes stronger and exhibits a blue shift under higher laser powers.

Ferroelectric properties of vertically aligned nanostructured BaTiO3-CeO2 thin films and their integration on silicon.

Epitaxial (BaTiO3)0.5(CeO2)0.5 films have been deposited in vertically aligned nanocomposite form on SrTiO3/TiN buffered Si substrates to achieve high-quality ferroelectrics on Si.

Direct observation of Lomer-Cottrell locks during strain hardening in nanocrystalline nickel by in situ TEM.

Strain hardening capability is critical for metallic materials to achieve high ductility during plastic deformation. A majority of nanocrystalline metals, however, have inherently low work hardening capability with few exceptions. Interpretations on work hardening mechanisms in nanocrystalline metals are still controversial due to the lack of in situ experimental evidence.

High quality p-type Ag-doped ZnO thin films achieved under elevated growth temperatures.

By correlating the effects of substrate temperature, oxygen pressure and laser energy on the electrical and microstructural properties of Ag-doped ZnO films grown on a sapphire (0001) substrate, p-type conductivity is achieved under various substrate temperatures in the wide range of 250-750 °C. All of the samples were deposited by pulsed-laser deposition under various designed conditions. Hall measurements indicate that the best conductivity is achieved in Ag-ZnO films under a substrate temperature of 500 °C, a partial oxygen pressure of 250-300 mTorr and laser energy between 330 and 345 mJ.

Epitaxial superconducting δ-MoN films grown by a chemical solution method.

The synthesis of pure δ-MoN with desired superconducting properties usually requires extreme conditions, such as high temperature and high pressure, which hinders its fundamental studies and applications. Herein, by using a chemical solution method, epitaxial δ-MoN thin films have been grown on c-cut Al(2)O(3) substrates at a temperature lower than 900 °C and an ambient pressure. The films are phase pure and show a T(c) of 13.

Self-separated PZT thick films with bulk-like piezoelectric and electromechanical properties.

Self-separated Pb(Zr(0.52)Ti(0.48))O(3) (PZT) films were processed by a hydrothermal deposition and a rapid thermal separation method, followed by a sol-gel filling and sintering process.

A novel organophosphorus hydrolase-based biosensor using mesoporous carbons and carbon black for the detection of organophosphate nerve agents.

To detect organophosphate chemicals, which are used both as pesticides and as nerve agents, a novel biosensor based on organophosphorus hydrolase was developed. By using mesoporous carbon (MC) and carbon black (CB) as an anodic layer, the sensitivity of the sensor to p-nitrophenol (PNP), which is the product of the organophosphorus hydrolase reaction, was greatly improved. The MC/CB/glass carbon (GC) layer exhibited an enhanced amperometric response relative to a carbon nanotube (CNT)-modified electrode because it promoted electron transfer of enzymatically generated phenolic compounds (p-nitrophenol).

Growth-controlled surface roughness in Al-doped ZnO as transparent conducting oxide.

The surface morphology of Al(2)O(3)-doped ZnO (AZO, 2 wt%) thin films varies from a uniform layer to nanorod structure by simply controlling oxygen pressure during growth. All AZO films were deposited on sapphire(0001) substrates using a pulsed laser deposition (PLD) technique. In the low oxygen pressure regime (vacuum approximately 50 mTorr), AZO films grow as a smooth and uniform layer.

A convenient synthesis of alpha-methylene-gamma-butyrolactones from allenyl carbonyl units mediated by Mo(CO)6 through intramolecular cyclocarbonylation.

A novel procedure for the synthesis of cis-fused bicyclic alpha-methylene-gamma-butyrolactones from allenyl carbonyl functionalities via the molybdenum-mediated cyclocarbonylation is described. The use of Mo(CO)(6) with DMSO to promote reaction results in an efficient and convenient protocol through the three-component assembly in high yields.

Silylative carbocyclization of allenyl-carbonyl units with Et3SiH catalyzed by rhodium: cis-stereoselective synthesis of homoallylic cycloalkanols.

[reaction: see text] A new procedure for the synthesis of cis-2-triethylsilylvinyl-cyclopentanols and -cyclohexanols from allenyl-aldehydes and -ketones with Et(3)SiH through rhodium-catalyzed silylative carbocyclization is described. The use of Rh(acac)(CO)(2) (1 mol %) to promote the reaction results in a mild and convenient protocol for the three-component assembly.