Zur Synthese von Human-Big-Gastrin I

The synthesis of the tetratriacontapeptide amide corresponding to the revised primary structure of human big gastrin I is described. For this purpose the fragments were designed in view of the maximum use of those utilized in our previous synthesis of human big gastrin I according to the first sequence proposal. Consequently the key tripeptide-Pro-Pro-His- (sequence 7–9) was prepared in suitably protected form to be used as amino or carboxyl component for assembly of the segments 1–9 and 1–14, respectively. Final condensation of the latter nona- and tetradecapeptide derivatives with the C-terminal segments 10–34 and 15–34 via the azide and the dicyclohexylcarbodiimide/N-hydroxysuccinimide procedure, respectively, leads to crude fully protected human big gastrin I. Upon deprotection by exposure to trifluoroacetic acid in presence of ethanedithiol-(1,2) as scavanger, ion exchange chromatography and partition chromatography, the desired tetratriacontapeptide amide was isolated in satisfactory yield with a high degree of purity. The identical immunological behaviour of the synthetic material, if compared with that of natural human big gastrin I, represents ulterior strong evidence for the correctness of the newly proposed structure for this putative prohormonal form of the gastrins.

Kurzmitteilung:Wünsch E., Wendlberger G., Mladenova-Orlinova L., Göhring W., Jaeger E., Scharf R., Gregory R. A., Dockray G. J., Hoppe-Seyler's Z. Physiol. Chem.362, 179 (1981).     

New Methods for the Synthesis of Glycosides and Oligosaccharides—Are There Alternatives to the Koenigs-Knorr Method? [New Synthetic Methods (56)]

Glycoproteins, glycolipids, and glycophospholipids (glycoconjugates) are components of membranes. The oligosaccharide residue is responsible for intercellular recognition and interaction; it acts as a receptor for proteins, hormones, and viruses and governs immune reactions. These significant activities have stimulated interest in oligosaccharides and glycoconjugates. With their help it should be possible to clarify the molecular basis of these phenomena and to derive new principles of physiological activity. Major advances in the synthesis of oligosaccharides have been made by the use of the Koenigs-Knorr method, in which glycosyl halides in the presence of heavy-metal salts are employed to transfer the glycosyl group to nucleophiles. The disadvantages of this procedure have led to an intensive search for new methods. Such methods will be discussed in this article. Emphasis is placed on glycoside and saccharide formation by 1-O-alkylation, on the trichloroacetimidate method, and on activation through the formation of glycosylsulfonium salts and glycosyl fluorides.     

一种无人机扩频遥控系统的性能分析

在剖析无人机扩频遥控系统组成的基础上,对无人机扩频遥控系统的处理增益、抗干扰容限及保密性能做了具体的分析,对无人机扩频遥控系统的雷达截获概率做了深入的探讨。     

太赫兹CSAR运动目标距离速度估计与重定位方法

圆周合成孔径雷达(CSAR)中,由于雷达平台绕观测场景圆周飞行,雷达和地面目标之间的距离方程复杂,目标的距离向参数和方位参数之间有复杂的耦合关系,导致单独估计动目标距离向速度参数的难度加大。提出一种基于子孔径分解的太赫兹CSAR运动目标距离向速度估计方法,选择合适的子孔径角度,对CSAR进行子孔径分解,在子孔径条件下,通过小角度近似,可以实现运动目标距离向速度和其他参数间的解耦合,准确估计运动目标的距离向速度,实现运动目标的精确重定位。仿真和实测数据验证了该算法的有效性。     

Divergent synthesis of 6H-isoindolo[2,1-a]indol-6-ones and indenoindolones: an investigation of Pd-catalyzed isocyanide insertion

A novel Pd-catalyzed intramolecular cyclization via tert-butyl isocyanide insertion from 2-(2-bromophenyl)-1H-indoles has been developed, which demonstrates the utility of isocyanides in C–N or C–C bond construction. Treatment of 2-(2-bromophenyl)-1H-indoles with tert-butyl isocyanide affords 6H-isoindolo[2,1-a]indol-6-ones with high efficiency. However, N-methyl or N-Boc protected 2-(2-bromophenyl)-1H-indoles gives indenoindolones in excellent yields under the same condition, which reveals that under the described situation, isocyanides insertion for the formation of C–N bonds is prior to that of C–C bonds.     

Synthesis of a furano abietane cyano enone—A new scaffold for biological exploration

A six step synthesis of furano abietane cyano enone 12 is described, in which the key step is a palladium-catalyzed intramolecular Heck reaction of bromo 3-phenoxyacrylate 17, prepared from enone phenol 13 in high yield.     

Synthetic strategies to 2′-hydroxy-4′-methylsulfonylacetophenone,a key compound for the preparation of flavonoid derivatives

Different strategies for the synthesis of 2′-hydroxy-4′-methylsulfonylacetophenone are reported in the present paper. This compound is considered as a key synthon for the synthesis of new flavonoid derivatives designed as potential cyclooxygenase-2 inhibitors. The retrosynthetic approach via 3′-methylsulfonylacetophenone, which included three synthetic pathways, did not allow us to obtain the expected compound. However, a synthesis from 3-mercaptophenol led to the desired acetophenone in three steps: thiophenol methylation, Friedel–Crafts acetylation and oxidation of the sulphide to the corresponding sulfone. The desired compound, 2′-hydroxy-4′-methylsulfonylacetophenone, will be used as a synthon for the preparation of novel flavonoid derivatives, such as 2′-hydroxychalcones, flavanones, flavones, and flavonols.     

A new algorithm of the nonlinear adaptive interpolation

The paper presents a new algorithm of NonLinearly Adaptive Interpolation （NLAI）. NLAI is based on both the gradients and the curvature of the signals with the predicted subsection, it is characterized by adaptive nonlinear interpolation method with extracting the characteristics of signals, Experimental research testifies the validity of the algorithm using the echoes of the Ground Penetrating Radar （GPR）. A comparison of this algorithm with other traditional algorithms demonstrates that it is feasible.     

IR Properties of Randomly Sea Surfaces

Sea surfaces should be considered as randomly rough surfaces at the infrared(IR) and optical bands. The geometric model of sea surfaces has been obtained by using image processing. Based on the electromagnetic scattering theory, the Laser Radar Cross Section(LRCS) for the sea surfaces is analyzed at IR band and the scattering properties of the sea surfaces have been gotten.