Two new terpenes from Tripterygium wilfordii

<正>Two new terpenes,wilfornine H(1) and triptobenzene Q(2) were isolated from Tripterygium wilfordii,as well as 11 terpenes. Their structures were elucidated by spectroscopic methods.Compounds 5,9-13 showed significant immunosuppressive activities.     

Short syntheses of (−)-clavaminol A and deacetyl (+)-clavaminol H

Concise stereoselective syntheses of (?)-clavaminol A and deacetyl (+)-clavaminol H have been achieved from simple starting materials. Highlights of the synthesis for (?)-clavaminol A include a highly diastereoselective chelation-controlled hydride reduction of an amino ketone to give the anti amino alcohol directly, and NaBH₄-mediated dehalogenation. The main synthetic approach for deacetyl (+)-clavaminol H features a highly diastereoselective chelation-controlled hydride reduction of the amino ketone to construct the anti amino alcohol and a palladium catalyzed hydrogenation reaction at the final step.     

Studies on pharmacokinetics,body distribution,plasma protein binding rate,and excretion of 1-methyl hydantoin in rats in vivo

In this paper, plasma concentration, plasma protein binding rate, body distribution, and excretion of both oral and intravenous administration of rats were determined by high performance liquid chromatography (HPLC) combining with UV detector. The blood drug concentration of oral and intravenous administration was summarized. The bioavailability of T_1/2 was approximately 0.75?hr. At the meanwhile, the bioavailability was about 18.84?±?2.21%. The plasma protein binding rate of 1-methyl hydantoin was about 24.36?±?0.93%, belonging to low protein binding drug. The result shows that 1-methyl hydantoin can be rapidly distributed in various organs and tissues and quickly eliminated within 6?hr without accumulation in the organs. Its discharge from the urine and feces was 16.58?±?4.48% and 3.37?±?0.71%, respectively. All of the results showed that the recovery rate, liner relationship, specificity, stability, and precision of the method were good. The study also proved that 1-methyl hydantoin has been eliminated quite faster in rats.     

单位球面中子流形一类抽象Willmore型泛函的变分问题

对于单位球面中的扎维子流形,本文构造一类抽象的W_((n,F))-Willmore型泛函,此泛函推广经典的Willmore泛函到相当一般的情形,它的临界点称为W_((n,F))-Willmore型子流形,本文计算泛函的变分公式,推导泛函临界点的Simons型不等式,针对特殊的函数F,构造W_((n,F))-Willmore型子流形的例子,最后给出泛函临界点间隙现象的刻画.     

Rate and Product Studies in the Solvolyses of Two Cyclic Phosphorochloridate Esters

Kinetic and product studies of the solvolyses of acyclic phosphorochloridates are extended to two cyclic diesters, 2-chloro-1,3,2-dioxaphospholane-2-oxide (1) and 2-chloro-5,5-dimethyl-1,3,2-dioxaphosphorinane-2-oxide (2). Slightly faster solvolyses are observed for 1 than for the acyclic dimethyl phosphorochloridate (3), and 2 solvolyzes somewhat slower than 3. An extended Grunwald–Winstein equation treatment shows similar sensitivities to changes in solvent nucleophilicity and solvent ionizing power for 1, 2, and 3, and a concerted S_N2 attack is proposed in each case. Product studies for the solvolyses of 2 in aqueous alcohols are presented.

     

STABILITY OF Se - Tl SCHOTTKY JUNCTIONS

Abstract

Evaporation of thallium on a crystallized layer of selenium results in an excellent Schottky diode, exhibiting a forward-to-reverse current ratio at 1 volt of some four to five orders of magnitude and a forward ideality factor close to unity. However, with the passage of time, there is a degradation in these electrical characteristics, if the thallium is exposed to the atmosphere, even at room temperature. The observed changes are a progressive increase in series resistance and a decrease in parallel capacitance. However, the changes with time can be greatly reduced if the thallium is covered with an evaporated film of Wood's metal. X-ray diffraction analysis of films of thallium deposited on glass substrates, shows that after prolonged exposure to air, the film is progressively transformed into Tl₂CO₃ . Oxide formation is only apparent after storage in oxygen, rather than air. The electrical degradation in the diodes is thus the result of atmospheric conversion of metallic thallium into the less conducting carbonate.     

A Six-Coordinate Picrate Nickel(II) Complex Based on the V-Shaped Ligand 1,3-Bis (1-Benzylbenzimidazol-2-yl)-2-Thiapropane: Synthesis,Crystal Structure,Biological Activities

Abstract

A six-coordinate picrate nickel(II) complex based on the V-shaped ligand 1,3-bis(1-benzylbenzimidazol-2-yl)-2-thiapropane (L), with the composition [Ni(L)₂](pic)₂, has been synthesized and characterized systematically. The crystal structure of the Ni(II) complex is a six-coordinated octahedron, which is considerably close to ideal octahedral geometry with N₄S₂ donors of the two ligands. Biological activities of compounds were investigated using electronic absorption spectroscopy, fluorescence spectroscopy, and viscosity measurements. The results suggested that both ligand L and Ni(II) complex bind to DNA in an intercalative binding mode, and DNA-binding affinity of the Ni(II) complex is stronger than that of ligand L.

[Supplementary materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements for the following free supplemental files: Additional figures.]     

Synthesis of some novel 5-substituted benzamido-6-arylamino-pyrazolo[3,4-D]pyrimidin-4-one derivatives for herbicidal activity

Abstract

Sixteen novel 3-methylthio-5-substituted benzamido-6-arylamino-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4 (5H)-one derivatives (4a–p) were successfully synthesized from iminophosphoranes, aryl isocyanate, and substituted benzoylhydrazine. The structures of the title compounds were elucidated by FT-IR, ¹H NMR, ¹³C NMR, and HRMS. Herbicidal activity of the compounds 4a–p against Brassica napus (rape), Echinochloa crusgalli (barnyard grass), Cucumis sativus (cucumber), and Triticum aestivum (wheat) were determined. The results showed that 5-(2-chlorobenzamido)-6-phenylamino-3-methylthio-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4 (5H)-one (4c) displayed remarkable inhibition activity against the stalk and root of rape with 100% inhibition rate at the dosages of 10?mg/L and 100?mg/L, and 5-(4-nitrobenzamido)-6-phenylamino-3-methylthio-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4 (5H) -one (4d) exhibited excellent activity against the stalk and root of barnyard grass with 100% inhibition rate at the same dosages.