Synthesis and antimycobacterial activity of purine conjugates with (S)-lysine and (S)-ornithine

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Directing-Group-Free C7-Alkylations of N-Alkylindoles Mediated by Cationic Zirconium Complexes: Role of Brønsted Acid for Catalytic Manifold

Highly position selective alkylations of N-alkylindoles at C7-positions have been enabled by cationic zirconium complexes. The strategy provides a straightforward access to install alkyl groups at C7-positions of indoles without a complex directing group. Mechanistic studies provided support for the importance of Brønsted acids in the catalytic manifold.     

Et2Zn-mediated stoichiometric C(sp)-H silylation of 1-alkynes and chlorosilanes

A first example of an Et₂Zn mediated silylation of 1-aklynes is reported. A series of functional groups are tolerated in this reaction. Mechanistic studies support Zn alkynilides as intermediates in the reaction. This reaction protocol provides a practical method for the preparation of alkynylsilanes and expands the application of organometallic zinc in organic synthesis.     

2,7-二氯荧光素与蛋白质相互作用的分光光度法研究

首次采用分光光度法研究了模拟生理条件(pH 7.4 Tris-HCl缓冲溶液,离子强度I=0.1)下2,7-二氯荧光素与牛血清白蛋白(BSA)相互作用的情况.研究结果表明:两者相互作用形成稳定的复合物,最大吸收波长为509nm,与2,7-二氯荧光素的最大吸收波长502nm比较,红移了7nm;两者之间主要通过静电引力结合,但并不排除疏水作用力和氢键;两者之间的结合数为32.     

3,7-二硝基亚氨基-2,4-二氮杂双环[3,3,0]辛烷的放热分解反应动力学

在程序升温条件下 ,用DSC研究了标题化合物的放热分解反应动力学 .用线性最小二乘法、迭代法以及二分法与最小二乘法相结合的方法 ,以积分方程、微分方程和放热速率方程拟合DSC数据 .在逻辑选择建立了微分和积分机理函数的最可几一般表达式后 ,用放热速率方程得到相应的表观活化能 (Ea)、指前因子 (A)和反应级数 (n)的值 .结果表明 :该反应的微分形式的经验动力学模式函数、Ea 和A值分别为 (1-α) 0 .44、2 30 .4kJ/mol和 10 18.16s-1.借助加热速率和所得动力学参数值 ,提出了标题化合物放热分解反应的动力学方程 .该化合物的热爆炸临界温度为 30 2 .6℃ .上述动力学参数对分析、评价标题化合物的稳定性和热变化规律十分有用 .     

Direct Observation of Non-covalent Complexes for Phosphorylated Flavonoid-protein Interaction by ESI

Diethyl flavon-7-yl phosphate was synthesized by modified Atheron-Todd reaction. The result of ESI shows that the phosphated flavonoids possess stronger binding affinities toward proteins such as myoglobin, insulin and lysozyme and are easier to form the non-covalent complexes with them.     

Mean value in invexity analysis

In this paper, a generalization of the mean value theorem is considered in the case of functions defined on an invex set with respect to η (which is not necessarily connected).     

硼砂与氯化铵合成hBN反应机理的研究

 研究了以硼砂、氯化铵为原料在氨气气氛下合成hBN 的反应机理。指出氯化铵在反应中的主要作用是与硼砂反应形成可阻止硼砂颗粒团聚的高熔点膜层；而氨气的主要作用就是提供大量参与反应的NH₃分子，增加了反应几率；新生成的hBN则进一步隔离高度熔融的硼砂团粒，防止玻璃相的生成。     

Dimethylamino-substituted 7H-Benzo[de]pyrazolo[5,1-a]isoquinolin-7-ones and Their Behavior under Vilsmeier-Haack Conditions

The behavior of dimethylamino-substituted 7H-benzo[de]pyrazolo[5,1-a]isoquinoline-7-ones, synthesized for the first time, under conditions of the Vilsmeier-Haack reaction. It has been shown that, on heating with POCl₃ and DMF, they are converted by electrophilic substitution at the position ortho to the dimethylamino group, followed by cyclization of the iminium adduct to a quinazolinium salt. When an acetyl group is present, the Arnold reaction, leading to the formation of a chloroaryl, accompanies the heterocyclization. The rates and proportion of the reaction products depend on the position of the dimethyl groups relative to the pyrazole ring.