Synthesis of dipyrrolo-diazepine derivatives via intramolecular alkyne cyclization

A regioselective approach was developed for the synthesis of dipyrrolo-diazepine derivatives. The synthetic route to dipyrrolo-diazepines first involves the synthesis of dipyrromethanes, followed by reaction of propargyl bromide in the presence of NaH to attach one alkyne functionality to the pyrrole nitrogen atom. Intramolecular heterocyclization with NaH in DMF between the alkyne functionality and pyrrole nitrogen atom gave the desired structures in good yields.     

Analysis of Solvent Effect on Mechanical Properties of Poly(ether ether ketone) Using Nano-indentation

Poly (ether ether ketone)(PEEK) is a high-performance semi-crystalline thermoplastic polymer.Exposure of the polymeric surface to solvents can have a strong effect like softening/swelling of polymeric network or dissolution.In this study, nano-indentation analysis was performed to study the effect of acetone on the surface mechanical properties of PEEK using different exposure time.The experiments were performed with a constant loading rate (10 nm/s) to a maximum indentation displacement (1000 nm).A 30-second hold segment was included at the maximum load to account for any creep effects followed by an unloading segment to 80% unloading.The indentation hardness and the elastic modulus were computed as a continuous function of the penetration displacement in the continuous stiffness mode (CSM) indentation.The experimental data showed that the peak load decreased from ~5.2 mN to ~1.7 mN as exposure time in solvent environment increased from 0 to 18 days.The elastic modulus and the hardness of PEEK samples also displayed a decreasing trend as a function of exposure time in the solvent environment.Two empirical models were used to fit the experimental data of hardness as a function of exposure time which showed a good agreement with the experimental values.     

PHOTOREACTIVITY OF 5-GERANOXYPSORALEN AND LACK OF PHOTOREACTION WITH DNA

5-Geranoxypsoralen, commonly called bergamottin, a major furocoumarin contained in bergamot oil, is reported in vitro as a highly photoreactive psoralen. In ethanol, it exhibits quite a high triplet state quantum yield (approximately 0.37). The triplet state is involved in subsequent photochemistry which depends on the initial concentration and on the presence of oxygen. In contrast to most psoralens, absorption and fluorescence data suggest that 5-geranoxypsoralen does not interact with DNA in the dark. No UVA-induced interstrand cross-links in DNA were shown.     

Picosecond Soliton Pulse Generation with a Zinc Phthalocyanine Thin-Film Saturable Absorber Via Mode Locking in an Erbium-Doped Fiber Laser Cavity

Journal of Russian Laser Research - In this paper, we employ a Zinc Phthalocyanine (ZnPc) organic material to construct a saturable absorber (SA) that is used in a laser cavity to generate...     

Micro-displacement sensor with multimode fused coupler and concave mirror

Fiber optic displacement sensor is demonstrated using a multimode fused coupler probe and a concave mirror target. It is observed that a focal length of the concave mirror make a significant influence to the displacement response, which illustrates three linear slopes with the second slope peaks at the position that is in vicinity of two times of the focal length. The highest sensitivity of 0.56 mV/mm is obtained with an infinity focal length and it is decreased as the focal length of the concave mirror decreases. The widest linear range of approximately 3.3 mm is observed in the third slope region with focal length of 6.0 mm. The highest linear range obtained with the use of 50:50 coupler.     

Numerical simulation of magnetohydrodynamic buoyancy-induced flow in a non-isothermally heated square enclosure

Numerical simulation of magnetohydrodynamic (MHD) buoyancy-induced heat transfer and fluid flow has been analyzed in a non-isothermally heated square enclosure using finite volume method. The bottom wall of enclosure were heated and cooled with a sinusoidal function and top wall was cooled isothermally. Vertical walls of the enclosure were adiabatic. Effects of Rayleigh number (Ra = 10⁴, 10⁵ and 10⁶), Hartman number (Ha = 0, 50 and 100) and amplitude of sinusoidal function (n = 0.25, 0.5 and 1) on temperature and flow fields were analyzed. It was observed that heat transfer was decreased with increasing Hartmann number and decreasing value of amplitude of sinusoidal function.     

The effects of a high-frequency suppressor on tuning curves and derived basilar-membrane response functions

Forward-masked psychophysical tuning curves were obtained using a fixed, low-level signal at a frequency of 4 kHz, and masker frequencies of 2.0, 2.5, 3.0, 3.5, 3.75, 4.0, 4.25, 4.5, 4.75, 5.0, and 5.5 kHz, at masker-signal gaps of 20, 30, 40, 60, 80, and 100 ms. An adaptive two-interval, two alternative forced-choice (21-2AFC) procedure was used to obtain the masker level at threshold. This procedure was repeated with the addition of a 4.75-kHz suppressor at 50 or 60 dB SPL, gated with the masker. Tuning curves were broader, and estimates of compression and gain from derived input/output functions were decreased in the presence of a suppressor as compared to the no-suppressor condition. The results are consistent with physiological results, which show that suppression leads to a broadening of tuning curves and a partial linearization of the midlevel portion of the basilar-membrane input/output function.     

First natural urease inhibitor from Euphorbia decipiens

Three new diterpene esters with a myrsinol-type skeleton have been isolated from Euphorbia decipiens BOISS. & BUHSE. The structure elucidation of the isolated compounds was based primarily on two-dimensional (2D)-NMR techniques including correlation spectroscopy (COSY), heteronuclear multiple quantum coherence (HMQC), heteronuclear multiple bond correlation (HMBC) and nuclear Overhauser effect spectroscopy (NOESY) experiments. Compounds 1 and 3 are active against prolyl endopeptidase and compound 2 showed inhibitory activity against urease enzyme.     

Synthesis and properties of isoviagra. A 2‐methyl‐2H‐pyrazolo[4,3‐d]pyrirnidin‐7‐one isomer of viagra®

The synthesis and spectral properties (ir, ms, nmr) of a substituted 2‐methyl‐2H‐pyrazolo[4,3‐d]‐pyrimidin‐7‐one ( 3 ), an isomer of Viagra^®, are described. The key synthon, 4‐amino‐1‐methyl‐5‐propyl‐3‐pyrazolecarboxamide ( 7 ), is prepared via the reaction of ethyl 2,4‐dioxoheptanoate with methylhydrazine, followed by cyclization, nitration, amidation, and nitro group reduction. Interaction of 7 with 2‐ethoxyben‐zoyl chloride yielded the respective bis‐amide ( 8 ) which was cyclized in polyphosphoric acid to the corresponding pyrazolo[4,3‐d]pyrimidin‐7‐one derivative 9 . Chlorosulfonylation of 9 , and subsequent treatment with 1‐methylpiperazine furnished iso Viagra ( 3 ).