Practical asymmetric amine nucleophilic approach for the modular construction of protected α-quaternary amino acids

We report the first amine nucleophilic approach for the modular construction of enantioenriched protected α-quaternary amino acids. The key to success is the use of an alcohol solvent, which makes a rationally designed COOMe-bonded Cu-allenylidene electrophilic intermediate stable enough to couple with amine nucleophiles before its decomposition. The reaction features wide functional group tolerance with high enantioselectivity, typically >90% ee, and is amenable to the modification of commercially available bioactive molecules. The resultant protected α-amino acids could be readily converted into a number of precious enantioenriched amines featuring α-hindered tertiary carbon centers, which are otherwise synthetically quite challenging, including those of α-amino aldehyde, peptides or α-vinyl amino ester with >92% ee in excellent yields. This protocol could be utilized for the synthesis of the protected bioactive α-ethylnorvaline in 3 steps, a significant advancement in comparison to an 11-step sequence reported previously.

We report the first amine nucleophilic approach for the modular construction of enantioenriched protected α-quaternary amino acids.     

The Antioxidant and Hypolipidemic Effects of Mesona Chinensis Benth Extracts

In this study, the antioxidant and hypolipidemic effects of Mesona Chinensis Benth (MCB) extracts were evaluated. Seven fractions (F0, F10, F20, F30, F40, F50 and MTF) were obtained from the MCB ethanol extracts. Compared to the commercial antioxidants (vitamin C), MTF and F30 exhibited higher antioxidant activities in the antiradical activity test and the FRAP assay. The half-inhibition concentration (IC50) for MTF and F30 were 5.323 µg/mL and 5.278 µg/mL, respectively. MTF at 200 µg/mL significantly decreased the accumulation of TG in oleic acid (OA)-induced HepG2 cells and reversed the inhibitory effect of Compound C on AMPK (MTF and F30 significantly increased the glucose utilization of insulin-induced HepG2 cells). In addition, the components of MTF were identified by HPLC-MS, which were caffeic acid, quercetin 3-O-galactoside, isoquercetin, astragalin, rosmarinic acid, aromadendrin-3-O-rutinoside, rosmarinic acid-3-O-glucoside and kaempferol-7-O-glucoside. Through statistical correlations by Simca P software, it was found that the main antioxidant and hypolipidemic components of MCB might be caffeic acid, kaempferol-7-O-glucoside, rosmarinic acid-3-O-glucoside and aromadendrin-3-O-rutinoside, which may play important roles in the AMPK pathway. MTF and F30 in MCB could be potential health products for the treatment of hyperlipidemia.     

Design,Synthesis, and In Vitro and In Vivo Antifungal Activity of Novel Triazoles Containing Phenylethynyl Pyrazole Side Chains

A series of triazole derivatives containing phenylethynyl pyrazole moiety as side chain were designed, synthesized, and most of them exhibited good in vitro antifungal activities. Especially, compounds 5k and 6c showed excellent in vitro activities against C. albicans (MIC = 0.125, 0.0625 μg/mL), C. neoformans (MIC = 0.125, 0.0625 μg/mL), and A. fumigatus (MIC = 8.0, 4.0 μg/mL). Compound 6c also exerted superior activity to compound 5k and fluconazole in inhibiting hyphae growth of C. albicans and inhibiting drug-resistant strains of C. albicans, and it could reduce fungal burdens in mice kidney at a dosage of 1.0 mg/kg. An in vivo efficacy evaluation indicated that 6c could effectively protect mice models from C. albicans infection at doses of 0.5, 1.0, and 2.0 mg/kg. These results suggested that compound 6c deserves further investigation.     

激光扫描技术在靶场测试中的应用研究

为了解决光电类仪器在武器射击准确度和射击密集度的测试中遇到天空背景亮度不够,或弹丸口径小,弹道偏高而无法测试的问题,利用旋转棱镜使激光束在空中扫描,照亮弹丸表面,从而大大降低对光电传感器灵敏度的要求,使得该项测试工作不受天空背景条件的影响,并提高测试精度.     

双偏振结构保偏光纤偏振器的研制

提出了保偏光纤偏振器的一种串联结构,即双偏振结构,报道了研制的结果。并通过对单偏振结构和双偏振结构器件测试结果的比较,得出双偏振结构的保偏光纤偏振器可使器件达到高消光比,并且有稳定的温度特性。     

Average kinetic energy of ions ejected from pure Coulomb explosions of methane clusters

We use an electrostatic model to study the average kinetic energy of ions ejected from the pure Coulomb explosions of methane clusters (CA4)n (light atom A=H and D). It is found that the ratio of the average kinetic energy of the ions to their initial average electrostatic potential energy is irrelevant to the cluster size. This finding implies that as long as the ratio is given, the average kinetic energies of the ions can be simply estimated from their initial average electrostatic potential energies, rather than from the time- consuming simulations. The ratios for the different charge states of carbon ions are presented.     

Conversion of CO_2 and H_2 into propane over InZrO_x and SSZ-13 composite catalyst

Direct converting carbon dioxide into hydrocarbon fuels and value-added chemicals would offer a very attractive approach for efficient utilization of CO₂ as a carbon resource.Although,olefins,aromatics and gasoline have been successfully synthesized by CO₂ hydrogenation,highly selective conversion of CO₂ and H₂ into C₂₊hydrocarbon is still challenging due to a high C-C coupling barrier and inhibiting the production of other long-chain hydrocarbons.Here,we report a composite catalyst made of InZrO_x and SSZ-13 molecular sieve(InZrO_x+SSZ-13),which exhibits 74.5% propane selectivity at 623 K.The 8-MR micropores and the higher strength of the acid for SSZ-13 benefit the formation of propane.Compared with pure InO_x and m-ZrO₂ the composite oxide InZrO_x containing more oxygen vacancies,exhibits to be more readily reduced by H₂ and easier to adsorb and desorb CO₂ within the reaction temperature.All those could be beneficial to the activation and conversion of H₂ and CO₂.The catalytic performance of InZrO_x+SSZ-13 in CO₂ hydrogenation provides a potential for production of propane.     

Temperature and metal composition dependence of lateral photovoltaic effect in Al-Alq3/SiO2/Si structures

A series of Al=-（Alq3）l-x granular films is prepared on Si wafer with native oxide layer using co-evaporation technique. Large lateral photovoltaic effect （LPE） is observed, with an optimal LPV sensitivity of 75 mV/mm in x=0.35 sample. The dependence of LPE on temperature and A1 composition is investigated, and the possible mechanism is discussed.