两个具有PTP1B抑制活性的4-羟基丁内酯化合物的全合成研究

Two new naturally 4-hydroxylated butenolides were concisely synthesized in excellent enantiomeric purities. An aldol condensation and a Suzuki reaction served successfully as the key steps in the synthesis.     

Diffusion Mechanisms of Zeolite Catalysts

The diffusion mechanisms within zeolite catalysts, such as resistance to diffusion at pore mouths, configurational diffusion, adsorption-controlled diffusion, influence of co-existing molecules and pore blocking, were overviewed. Two kinds of diffusivities, the intracrystalline diffusivity and the effective diffusivity, were discussed separately to clarify the diffusion mechanism.     

固体超强酸催化下的醛酮自身缩合及其溶剂效应的研究

研究了在三种固体超强酸催化下醛(酮)自身的羟醛缩合反应,系统考察了反应时间,催化剂用量等因素对反应的影响,优化了反应条件.同时,对该反应的溶剂效应进行了研究.结果表明,当催化剂用量为2 g/1 mol醛(酮),反应5 h,转化率可达40%,溶剂对该反应有明显的抑制作用.超强酸对各种醛都具有较好的催化活性,其催化醛类化合物自身缩合的转化率都在48%以上,选择性在95%以上,证明固体超强酸对该缩合反应有较好的催化活性和选择性.     

Bismuth(III) nitrate pentahydrate—a mild and inexpensive reagent for synthesis of coumarins under mild conditions

Bismuth(III) nitrate pentahydrate is found to be an efficient catalyst for the Pechmann condensation reaction of phenols and β-ketoesters under solvent-free conditions. The reaction protocol is simple and is followed by aqueous work-up leading to the formation of the corresponding coumarin derivatives in good yield and high purity.     

Synthesis and Cytotoxic Activity of 4-Substituted 3-Cyano-6,6-dimethyl-5,6-dihydro-2-pyranones

The respective 4-(arylvinyl)lactones and compounds of the Michael adduct type were synthesized by the condensation of substituted benzaldehydes with 3-cyano-4,6,6-trimethyl-5,6-dihydro-2-pyranone in the presence of catalytic amounts of sodium hydroxide. It was shown by the semiempirical AM1 method that the indicated products can be formed through one and the same intermediate compound. Some of the synthesized phenylvinyl-5,6-dihydro-2-pyranones have a cytotoxic effect, and this corresponds to the prognosis of the OREX expert system.     

Propanal in the Syntheses of Alkyl-substituted 3-Cyano-2-piperidone, 3-Cyano-2,5,6,7-tetrahydropyrindin-2(1H)-one, and 3-Cyanopyridine-2(1H)-thione

Condensation of propanal with cyanothioacetamide and morpholine gave 3-cyano-4-ethyl-5-methyl-6-morpholino-2-piperidone, the structure of which was studied by X-ray analysis. Reaction of propanal with cyanothioacetamides and cycloalkanone enamines gave 3-cyano-4-ethyl-2,5,6,7-tetrahydropyrindin-2(1H)-one and 3-cyano-4-ethyl-5,6-hexamethylenepyridine-2(1H)-thione. The latter was used for the preparation of substituted 2-benzyloxycarbonylmethylthiopyridine and 3-amino-2-benzyloxycarbonylthieno[2,3-b]pyridine. __________ Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 7, pp. 1053–1059, July, 2005.     

Knoevenagel缩合反应研究的新进展

综述了近年来Knoevenagel缩合反应研究的新进展, 包括微波、超声波、固相合成、离子液体等新技术新试剂在该反应中的应用.     

An electrothermal vaporization unit with axially focusing convection upstream. Part II: Modeling of the condensation process

A model is presented that describes quantitatively the condensation of analytes in pico- and nanogram masses sampled with electrothermal vaporization (ETV). It presumes that the analyte vapor condensation of such low amounts occurs mainly heterogeneously, predominantly on growing carbon particulates originating from the graphite furnace before the analyte vapor achieves saturation via cooling. The model regards the coagulation of carbon particles and the diffusion of analyte atoms. The criterion whether or not an analyte atom sticks to a colliding particle is chosen as a function depending on its temperature and on the common GFAAS pretreatment temperatures. Heterogeneous condensation of six analytes with different volatilities, Ag, Cu, Fe, Ni, Mn, and Pb, is calculated for the ETV unit with an axially focusing convection upstream described in Part I. Modifier effects are taken into account. The results are compared to measured data.     

Production of submicron-size monodisperse polymer particles having aldehyde groups by the seeded aldol condensation polymerization of glutaraldehyde (II)

Submicron-size monodisperse polystyrene/polyglutaraldehyde (PS/PGLA) composite particles having aldehyde groups at the surfaces were produced by the seeded aldol condensation polymerization of glutaraldehyde at various temperatures of 040°C. Since a part of aldehyde groups was consumed by the Cannizzaro reaction (hemiacetal formation) as a intermolecular reaction of PGLA, the amount of aldehyde groups on PS/PGLA composite particles was varied by the competition between the aldol condensation reaction and the Cannizzaro reaction at the various temperatures.Part CXXXIX of the series Studies on Suspension and Emulsion     

Probing in vitro digestion at oil–water interfaces

Interfacial layers have been widely applied to study the formation and stability of emulsion-based systems. However, the application of isolated interfaces to address digestibility of emulsions is often limited because of the complexity of experimental methods and results. This review summarizes the latest developments in analytical methods and literature data on effects of digestion on interfacial layers. Particular emphasis is given to understand the changes on interfacial magnitudes during oral, gastric, and duodenal digestion, either applied separately or sequentially. Limitations of interfacial aspects and key factors that influence emulsion microstructure in bulk and lipid digestion are identified. Understanding the behavior of interfacial layers upon gastrointestinal digestion promotes an accurate tracking of the physiological fate of emulsions.