Vancomycin Analogues Containing Monosaccharides Exhibit Improved Antibiotic Activity: A Combined One‐Pot Enzymatic Glycosylation and Chemical Diversification Strategy

Many natural products contain carbohydrate moieties that contribute to their biological activity. Manipulation of the carbohydrate domain of natural products through multiple glycosylations to identify new derivatives with novel biological activities has been a difficult and impractical process. We report a practical one‐pot enzymatic approach with regeneration of cosubstrates to synthesize analogues of vancomycin that contain an N‐alkyl glucosamine, which exhibited marked improvement in antibiotic activity against a vancomycin‐resistant strain of Enterococcus.     

复合广义齐次Poisson过程的多险种破产概率

本文推广了经典的复合泊松风险模型，建立了两类复合广义齐次poisson过程的多险种破产模型．对于新模型，我们得到了初始资本为u的破产概率φ(u)的精确表达式以及特殊情况下φ(0)的表达式，并且导出了调节系数方程和调节系数R的上下界．     

Preparation of silane-grafted pellets: silica bound reagents in a very convenient form

High surface area silica pellets are excellent supports for the preparation of silica supported reagents and solid-phase basal linkers through reaction with (RO)₃Si(CH₂)₃FG (FG=NH₂, NHMe, Cl, NHC(O)NH₂, OC(O)CMe(CH₂), NCO, NEt₂). High loadings (0.66-2.15 mmol g⁻¹) of grafted silane materials are realised at synthetically useful loadings per pellet (ca. 0.06 mmol). Preliminary trials show that trial linker chemistry and ligand synthesis can be carried out on these materials and that these reactions can be monitored by solid state ¹³C NMR studies on individual pellets.     

过渡金属催化的1,6-烯炔环异构化反应

1,6-烯炔底物在过渡金属催化剂作用下的化学行为得到了广泛的研究,重点是关于过渡金属催化的1,6-烯炔环异构化反应.从反应机理角度入手,把1,6-烯炔环异构化反应按启动方式总结为三类,并对这三种方式启动的1,6-烯炔环异构化反应进行了详细地总结和阐述.     

An efficient phosphine-free palladium coupling for the synthesis of new 2-arylbenzo[b]thiophenes

Straightforward and rapid access to 2-arylbenzo[b]thiophenes has been developed. It involved a catalytic coupling of 3-activated benzo[b]thiophenes with several aryl halides in the presence of a phosphine-free palladium system. In case of fragile functional groups such as aldehydes, a quaternary ammonium was used as an additive as with the other substrates, the coupling performed better and faster in the presence of a crown ether, the best one being DCH-18-C-6, with good yields and low reaction times. This method would provide a direct access to novel structures of biological interest.     

The first encapsulation of hydroxynitrile lyase from Hevea brasiliensis in a sol-gel matrix

A straightforward process for the encapsulation of HbHNL under low methanol conditions has been developed. By adding a sol, prepared by hydrolysis of TMOS/MTMS at pH 2.8 with continuous removal of methanol, to a stirred solution of the enzyme in a buffer at pH 6.5, at least 65% of the activity of the free enzyme could be recovered after the encapsulation. The aquagels were successfully used in the synthesis of (S)-cyanohydrins.     

New characterizations of Hajlasz-Sobolev spaces on metric spaces

This paper introduces the fractional Sobolev spaces on spaces of homogeneous type,includingmetric spaces and fractals. These Sobolev spaces include the well-known Hajfasz-Sobolev spaces as specialmodels.The author establishes varions chaaracterizations of(sharp)maximal functions for these spaces.Asapplications,the author identifies the fractional Sobolev spaces with some Lipscitz-type spaces.Moreover;some embedding theorems are also given.