Anti-inflammatory, pro-proliferative and antimicrobial potential of the compounds isolated from Daemonorops draco (Willd.) Blume.

The invention provides a method for preparing phenol ether through the reaction of a phenolic compound and a halogenated hydrocarbon, and the method is a synthetic method which adds superfine potassium carbonate in reaction raw materials to replace traditional sodium alcoholate as a catalyst. The method comprises the following steps: adding the phenolic compound, the halogenated hydrocarbon and the superfine potassium carbonate into a reactor according to a certain proportion, simultaneously adding a C1-C4 low-carbon alcohol solvent and performing a reaction under stirring at the temperature of 30-80 DEG C; filtering after the reaction is completed, and recovering the solvent in filtrate by distillation to get a phenol ether product; and in addition, the phenol ether product can be purified by recrystallization and then an industrial product in the purity of above 98.5% can be obtained. The method is used for synthesizing phenol ether type compounds, side reactions caused by the use of the sodium alcoholate and other strong bases are avoided, and the yield of the phenol ether compounds is greatly improved; the potassium carbonate which is not reacted and potassium salts generated by reaction can be recovered by filtering; and the removal of the sodium alcoholate by water washing and other operations can be avoided, and industrial waste water can be reduced by 90%, so that the method has great industrial prospects.

Method for preparing phenol ether through reaction of phenolic compound and halogenated hydrocarbon

Two novel taspine diphenyl derivatives (Ta-dD) were designed and synthesized by introducing different coumarin fluorescent groups into the basic structure of Ta-dD. The main advantage of these two compounds is that they can be used as fluorescence probes and inhibitors simultaneously. In the present study, the fluorescent properties of the probes were measured and their inhibition of four breast cancer cell lines was tested. Different concentrations of the fluorescence probe were added to MCF-7 breast cancer cells for fluorescence imaging analysis under normal conditions. The results suggested that both of the new compounds have not only fluorescence but also the ability to inhibit effects on different breast cancer cell lines, which indicates their possible further use as dual functional fluorescence probes in tracer analysis. Copyright © 2011 John Wiley & Sons, Ltd.

Synthesis of novel taspine diphenyl derivatives as fluorescence probes and inhibitors of breast cancer cell proliferation.

The invention discloses a 2-benzyl-1-isoquinolone compound as well as a synthesis method and application thereof, and belongs to the technical field of pharmaceutical synthesis. According to a synthesis route of the 2-benzyl-1-isoquinolone compound, substituted 1-isoquinolone and substituted benzyl chloride react in dry DMF under the presence of sodium hydride, so as to generate the 2-benzyl-1-isoquinolone compound, wherein the substituted benzyl chloride is 4-methoxybenzyl chloride, 3,4-dimethoxybenzyl chloride or 3,4,5-trimethoxybenzyl chloride. Isolated arterial ring tension experiments prove that the 2-benzyl-1-isoquinolone compound with a concentration of 10 mol/L has an obvious function of relaxing the mesenteric arteries of an SD rat; intragastric administration to a spontaneously hypertensive rat proves that the 2-benzyl-1-isoquinolone compound has an obvious function of reducing blood pressure. Therefore, the 2-benzyl-1-isoquinolone compound can be applied to preparation of pharmaceutical preparations for treating cardiovascular diseases.

2-benzyl-1-isoquinolone compound as well as synthesis method and application thereof

N-acetyl-quinoline-2 (1H) ketone compounds as well as preparation method and application thereof

The invention discloses a synthesis method of 2-substituted-3, 4-dihyidro-1-isoquinoline ketone compound and a relative application in the drug preparation for cardiovascular disease, wherein the compound is represented as above, R1 is gaseous normal alkyl and aromatic group or various substituted alkyl and aromatic group of C1-C19, R2 is OH, OCH3, CH3, NO2 and halogen or the like and can be one or more substituents. The preparation of 2-substituted-3, 4-dihyidro-1-isoquinoline ketone compound uses isovanillic acid ester as raw material, via six-step reaction as allyl etherified, Claisen rearrangement, oxidation, reaction with primary amine (generating Schiff base), reduction and aminolysis of molecular lactone, to synthesize the product. The isolated arterial ring tension test proves that the compound can relax vessel effectively. The 2-substituted-3, 4-dihyidro-1-isoquinoline ketone compound is a new potential cardiovascular drug, with wide application for preparing the drug of cardiovascular disease.

Method for synthesizing 2-substituted-3,4-dihydro-1-isoquinoline ketones and use thereof for preparing cardiovascular agents

The facile and efficient total synthesis of taspine was achieved in 10 steps in high yield (16.5% overall) from commercially available isovanillin. Key steps in the synthesis are preparation of a symmetrical homodimer employing a classical Ullmann coupling reaction, and introduction of an allyl substituent by the Claisen rearrangement reaction. Significantly, the facile synthetic scheme proposed in this work has the characteristics of mild reaction conditions, inexpensive reagents, higher yield, and simple operation.

Qiang Li

Papers

Method for synthesizing 2-substituted-3,4-dihydro-1-isoquinoline ketones and use thereof for preparing cardiovascular agents

Facile and Efficient Total Synthesisof Taspine

Facile and Efficient Total Synthesis of Taspine.

Efficient Synthesis of Thalifoline and Its Analogues.