4-(7-Methoxy-2,2-dimethyl-2,3-dihydrobenzo-furan-5-yl)-N-(pyridin-2-yl)thiazol-2-amine: Chiral Crystal from Achiral Molecule

The title compound 4-（7-methoxy-2,2-dimethyl-2,3-dihydrobenzofuran-5-yl）-N- （pyridin-2-yl） thiazol-2-amine was synthesized by reacting 2-bromo-1-（7-methoxy-2,2-dime- thyl-2,3-dihydrobenzofuran-5-yl）ethanone with 1-（pyridine-2-yl）thiourea, and its crystal was determined by single-crystal X-ray diffraction. The crystal belongs to the monoclinic system, chiral space group C2 with a = 18.1328（14）, b = 5.5969（5）, c = 19.2195（15） A, β= 115.5420（10）°, V= 1759.9（2）A3, Z = 4, F（000） = 744, C19H19N3O2S, Mr= 353.43, Dc= 1.334 g/cm3, S = 1.15, μ = 0.201 mm-1, the final R = 0.035 and wR = 0.111 for 2307 observed reflections （I 〉 2σ（I））. The Flack parameter is -0.03（10）. The preliminary bioassay result indicated that the title compound exhibits strong insecticidal activity （93.75% mortality） against Mythimna separate at the concentration of 1.000 g/L.

Interaction of N-(2-Methyl Thio Phenyl)-2-Hydroxy-1-Naphthaldimine with Tin Dioxide Nanoparticles: A Spectroscopic Approach

The interaction of N-(2-methyl thiophenyl)-2-hydroxy-1-naphthaldimine (NMTHN) with tin dioxide nanoparticles (SnO2 NPs) has been investigated by spectroscopic tools such as absorption and fluorescence spectroscopy. Absorption spectroscopy reveals the formation of ground state complex. Fluorescence spectroscopy has been used to study the signatures of fluorescence quenching. SnO2 NPs are found to quench the intrinsic fluorescence of NMTHN via static and dynamic quenching. The deviation from linearity in the Stern-Volmer plot has been observed.

以甘油为碳源发酵高产反式-4-羟脯氨酸菌株的选育及营养优化

以低品级甘油为碳源进行微生物发酵合成反式-4-羟脯氨酸(Trans-4-hydroxy proline,Hyp)的探索。从实验室构建的重组菌E.coli BL21(DE3)/p UC19-ptrp2-Hyp出发,通过易错PCR随机突变和常压室温等离子体复合诱变处理,利用单菌落琼脂块和氨基酸显色相结合高通量筛选出1株以甘油为唯一碳源的Hyp高产菌P71。与葡萄糖培养基相比,该菌株更适合在甘油上生长并转化L-脯氨酸合成Hyp,发酵20 h产Hyp高达1.20g/L,比生长在葡萄糖培养基上高70%以上;比其出发菌株在葡萄糖培养基上产量提高了1倍以上。通过培养基成分系统优化,发现胰蛋白胨、Fe SO4和L-脯氨酸是3大主要影响因素,最适加量分别为7.01 g/L、11.51 g/L和1.41 mmol/L;在该条件下突变菌株摇瓶发酵12 h产Hyp达1.61 g/L,比优化前提高了50%。

Total Synthesis of (-)-Tetrahydrolipstatin by the Tandem Mukaiyama-aldol Lactonization

（-）-Tetrahydrolipstatin 1 was synthesized in three steps and 33.8% overall yield from aldehyde 6 by tandem Mukaiyama-aldol lactonization, which offered a concise, efficient and highly diastereoselective route to this antiobesity drug. We also presented a resolution method for preparation of the crucial intermediate, β- （t-butyldimethylsilyloxy）tetradecanal.

真菌来源的5-脂氧合酶抑制剂:Butyrolactones(英文)

我们在进行微生物来源的5-脂氧合酶抑制剂的筛选过程中,得到了一株具有活性的曲霉菌F06Z-509。经过对其发酵产物进行分离纯化,最终得到三个活性化合物,分别为F06Z-509-A,B和C。通过对它们核磁和质谱数据进行分析,确定其结构分别与已知化合物butyrolactoneⅡ,Ⅰ和Ⅲ相同。它们对5-脂氧合酶都表现出较强的抑制活性,IC_(50)值分别为21.43,22.51和11.83μg/mL。它们对5-脂氧合酶的抑制活性未见报道。

Asymmetric synthesis of syn-aryl-(2S,3R)-2-chloro-3-hydroxy esters via an engineered ketoreductase-catalyzed dynamic reductive kinetic resolution

We report here a generic,green synthesis of 17 valuable syn-aryl-(2S,3R)-2–chloro-3–hydroxy esters(syn-(2S,3R)-1)in 73%-99%isolated yields along with 6.1:1–83:1 dr and 31%~>99%ee,through dynamic reductive kinetic resolution of racemic arylα–chloroβ-keto esters(2)catalyzed by an engineered ketoreductase which was obtained via ep PCR-based directed evolution.The hectogram scale synthesis of syn-(2S,3R)-1b at a substrate concentration of 120 g/L showcased the application potential of the biocatalytic method developed presently.

MICROBIAL TRANSFORMATION OF 19-HYDROXY-CHOLESTEROL ACETATE OR 19-HYDROXY-β-SITOSTEROL ACETATE TO △~4-19-HYDROXY ANDROST-3, 17-DIONE

The increasing medicinal importance of 19-norsteroids, particularly for oral contraceptives, has stimulated intensive research to continuously find more economic methods of either partial and total direct synthesis or indirect synthesis via estrone of this class of compound.

高龄高血压患者血清维生素D3与外周动脉硬化的相关性分析

目的探讨高龄高血压患者血清维生素D3水平与外周动脉硬化的相关性。方法入选2011年9月至2012年11月在北京友谊医院老年科住院的高龄老年高血压患者166例,年龄75~99(85.5±4.9)岁。以血清25-羟基维生素D3[25(OH)D3]<20 ng/ml作为维生素D3缺乏的诊断标准,将患者分为维生素D3缺乏组(n=118)和维生素D3正常组(n=48)。动态血压及下肢动脉超声结果反映外周动脉硬化程度,分析维生素D3缺乏和外周动脉硬化的相关性。采用SPSS 16.0软件对数据进行统计分析。计量资料用均数±标准差(±s)表示,两组比较采用t检验。计数资料用百分率表示,组间比较用χ~2检验。Logistic回归分析下肢动脉狭窄的相关危险因素。结果相比维生素D3水平正常组,维生素D3缺乏组患者的LDL-C水平高,舒张压更低,脉压更大,高脂血症和外周动脉硬化发病率高,差异具有统计学意义(P<0.05)。Logistic回归分析结果表明下肢动脉狭窄与维生素D3水平(OR=0.780,95%CI 0.670~0.890;P=0.039)、舒张压水平负相关(OR=1.030,95%CI 0.929~0.983;P=0.040),而与LDL-C水平正相关(OR=2.446,95%CI 1.138~1.312;P=0·043)。结论高龄高血压患者血清维生素D3缺乏与外周动脉硬化有明显相关性。

披针叶茴香果实的化学成分研究

目的研究八角科（Illiciaceae）植物披针叶茴香（Illicium lanceolatum）果实的化学成分。方法应用硅胶、Sephadex LH-20、MCI等各种色谱技术进行分离纯化，根据化合物的理化常数和波谱数据鉴定其结构。结果从披针叶茴香果实的体积分数95％乙醇提取物中分离得到12个化合物，通过渡谱数据和理化常数分别鉴定为2，4-dihydroxy—allylbenzene-2-O-β-D—glucopyranoside（1），（＋）-儿茶素（2），槲皮素-3-O-β-L-鼠李糖苷（3），芦丁（4），异鼠李素-3-D-β-D-芸香糖苷（5），6-deoxy-1-hy—droxy neoanisatin（6），莽草毒素（7），icarisideE3（8），（75，8R）-urolignoside（9），对羟基苯甲酸（10），莽草酸（11），β-谷甾醇（12）。结论化合物1，4～6，8～10为首次从该植物中分离得到。