34 results about "Phenylpropiolic acid" patented technology

Cinnamic and phenylpropiolic acid derivatives of Formula (I) having antitumour and chemosensitizing activity are described. Also described are pharmaceutical compositions containing the above-mentioned compounds, for the treatment of tumours.

The invention discloses a hyperbranched polyphenyltriazole formate, a preparation method and application thereof. Using phenylpropiolic acid tribasic ester and binary organic azide monomer, in polar aprotic solvent, heating and reacting for a period of time to obtain hyperbranched polyphenyltriazole formic acid ester. The reaction raw materials in the present invention are easy to obtain, and no by-products are generated during the polymerization process, which conforms to atom economy. The substrate of the polymerization reaction has a wide range of applications, has good compatibility with functional groups, and can easily introduce functional groups. At the same time, no metal catalyst is used in the preparation process of the polymer, which avoids the impact of catalyst residue on the biological activity and photoelectric performance of the polymer. Because the polymer contains a tetraphenylethylene structure, the polymer has good aggregation-induced luminescent properties, and can be used as a chemical sensor to detect polynitroaromatic explosives with high sensitivity.

A compound represented by the following general formula (1) or a salt thereof, which has superior inhibitory activity against type 4 PLA2, and thus has prostaglandin and / or leucotriene production suppressing action [X represents a halogen atom, an alkyl group which may be substituted, or the like, Y represents hydrogen atom or an alkyl group which may be substituted, and Z represents hydrogen atom or an alkyl group which may be substituted].

The invention relates to the field of chemical synthesis, in particular to a preparation method of neoflavonoids. The preparation method is characterized by comprising the following steps of using substituted benzaldehyde as an initial raw material to be reacted with malonic acid to generate a substituted phenylacrylic acid compound; performing an addition reaction, an elimination reaction and the like on the substituted phenylacrylic acid compound, or performing acetylation so as to protect a phenolic hydroxyl group, then performing a bromination reaction and the elimination reaction so as to synthesize the substituted phenylpropiolic acid compound ; and using montmorillonite K-10 after being acidulated by sulfuric acid as a catalyst, enabling the substituted phenylpropiolic acid compound and a phenolic compound to perform a heating reaction so as to generate the neoflavonoids. Compared with the prior art, the preparation method of the neoflavonoids, disclosed by the invention, has the characteristics that raw materials are cheap, and easy to obtain, the operation is simple, the catalyst can be recovered for use, and the method is environmentally-friendly, the post-treatment is simple, and the production cost is low, and the method has a high popularization and application value.

The invention discloses an aryl-alkyne compound (2,3,6,7-tetrahydro-1H,5H-pyrido[3,2,1-ij]quinolin-8-yl 3-phenylpropiolate) as well as preparation and application of the compound. A synthesis method of the aryl-alkyne compound comprises the following steps: under the condition that the temperature is 0 DEG C, dissolving 8-hydroxyjulolidine and phenylpropiolic acid into dichloromethane and adding a condensing agent EDC (Ethylene Dichloride) and an alkali DMAP (Dimethylaminopyridine) and stirring and reacting at 20 to 30 DEG C for 5 to 8 hours; after the reaction, concentrating; carrying out silica-gel column chromatography on concentrated liquid; then eluting, decompressing and evaporating to remove the solvent to obtain a product. The compound can be used as a reagent for detecting the concentration of trivalent gold ions by a fluorescent spectrometry. Firstly, the aryl-alkyne compound provided by the invention has a simple preparation method and low cost and is prepared from the 8-hydroxyjulolidine and the phenylpropiolic acid through a one-step reaction; secondly, the compound can be used as a trivalent gold detection reagent and has high sensitivity and selectivity on Au<3+>; a detection result is not interfered by other metal ions; a detection method is simple and a detection process is carried out in a water phase and can be realized with the help of a fluorescence spectrophotometer.

The invention discloses a 4-aryl coumarin compound and a preparation method and application thereof. The 4-aryl coumarin compound has a structure shown in a formula (I). The preparation method comprises the following steps: taking substituted benzaldehyde and propandioic acid as raw materials, heating under condition of existing pyridine and piperidine, and generating Perkin reaction and decarboxylic reaction to obtain a series of substituted phenylacrylic acid compounds; carrying out bromination and elimination reaction on the substituted phenylacrylic acid compounds or acetylation to protect a phenolic hydroxyl group, and then carrying out bromination and elimination reaction to obtain substituted phenylpropiolic acid compounds; and enabling the substituted phenyl propargylic acid compounds and phenolic compounds to react under the catalysis of boron trifluoride etherate and phosphorus oxychloride or trifluoroacetic acid to obtain a series of 4-aryl coumarin compounds. The compounds can be used for preparing antineoplastic medicine, anti-abnormal-angiogenesis medicine, antimicrobial medicine, antioxidation medicine and antimalarial medicine.

The invention discloses a method for preparing alpha-alkynyl substituted ether compounds. The method comprises the following steps: taking propiolic acid as a raw material, and synthesizing substituted phenylpropiolic acid under conditions of substituted iodobenzene, 1,8-diazabicyclo[5.4.0]undec-7-ene, (beta-4)-platinu and dimethyl sulfoxide; taking substituted phenylpropiolic acid and p-bromophenol as raw materials, and synthesizing p-bromophenyl substituted phenylpropiolic acid ester under the conditions of 4-dimethylaminopyridine and N,N'-Dicyclohexylcarbodiimide; and performing an alkynylation reaction on the p-bromophenyl substituted phenylpropiolic acid ester in participation of tert-butyl hydroperoxide, cesium carbonate and tetrahydrofuran, and finally synthesizing alpha-alkynyl substituted ether products. According to the method disclosed by the invention, simple and readily available acetylene esters serve as an alkynylation reagent, and the target products, namely alpha-alkynyl substituted ether compounds, are synthesized in a green and environmental-friendly manner under mild conditions. The compounds play an important role in construction of multiple medical intermediates and bio-active structures.

The invention provides a method and system for preparing phenylpropionic acid. The phenylpropionic acid preparation method comprises the following steps of: putting an amino acid solution and a dissolving agent into a reaction tank, dissolving, stirring, reacting and standing; adding a PH regulator into the reaction tank and heating and stirring until the current PH value of the solution in the reaction tank is equal to a PH threshold value; adding phenylpropanal and a catalyst into the reaction tank, and continuously injecting oxygen to control oxidation reaction between the phenylpropanal and the oxygen; continuously heating the reaction tank and when the current temperature in the reaction tank is equal to a temperature threshold value, continuously heating the reaction tank at the temperature threshold value until the phenylpropanal is completely oxidized to obtain crude phenylpropionic acid; injecting the crude phenylpropionic acid into a low-pressure separation tank for low-pressure separation, and heating and rectifying the separated crude phenylpropionic acid to obtain refined phenylpropionic acid. The phenylpropionic acid preparation method and the phenylpropionic acid preparation system have the advantages of convenience in operation, flexibility in use and high preparation stability.

The invention discloses a method for preparing alpha-alkynyl substituted ether compounds. The method comprises the following steps: taking propiolic acid as a raw material, and synthesizing substituted phenylpropiolic acid under conditions of substituted iodobenzene, 1,8-diazabicyclo[5.4.0]undec-7-ene, (beta-4)-platinu and dimethyl sulfoxide; taking substituted phenylpropiolic acid and p-bromophenol as raw materials, and synthesizing p-bromophenyl substituted phenylpropiolic acid ester under the conditions of 4-dimethylaminopyridine and N,N'-Dicyclohexylcarbodiimide; and performing an alkynylation reaction on the p-bromophenyl substituted phenylpropiolic acid ester in participation of tert-butyl hydroperoxide, cesium carbonate and tetrahydrofuran, and finally synthesizing alpha-alkynyl substituted ether products. According to the method disclosed by the invention, simple and readily available acetylene esters serve as an alkynylation reagent, and the target products, namely alpha-alkynyl substituted ether compounds, are synthesized in a green and environmental-friendly manner under mild conditions. The compounds play an important role in construction of multiple medical intermediates and bio-active structures.

The invention discloses a 3-sulfone-based coumarin and a preparation method thereof. The method of the invention is to react an aromatic amine, phenyl phenylpropiolate and serotonin in an organic solvent to prepare a 3-sulfone-based coumarin elemental compounds whose structures have been 1 H NMR, 13 Characterized and confirmed by C NMR, HRMS and other methods. The method of the present invention reacts under mild conditions, and utilizes diaoba block as a source of sulfur dioxide to directly realize the sulfonylation reaction and construct a 3-sulfone-based coumarin compound; the conversion reaction raw materials are simple and easy to obtain, and the traditional synthesis method is avoided The use of medium sulfonyl chloride is suitable for large-scale preparation and has very good application prospects.

The invention discloses a method for preparing an indolone derivative. The method disclosed by the invention comprises the step of subjecting phenylpropiolic acid and aniline, which serve as startingraw materials, to four steps, i.e., condensation, nucleophilic substitution, palladium catalyzing coupling and hydrolyzing sequentially, thereby obtaining the indolone derivative. According to the method disclosed by the invention, the raw materials are readily available, the operation is simple and convenient, the production efficiency is high, enlarged production is facilitated, and the productis high in total yield and easy to purify.

The invention discloses a method for catalyzing decarboxylation coupling reaction by a 1,2,3-triazole monosubstituted 1,3,5-s-triazine compound coordinated with CuSO4.5H2O. By taking CuSO4.5H2O which is good in stability and cheap and easily available and the triazine compound which is stable in water and air and high in functionalization as a catalytic system, the method catalyzes decarboxylation coupling reaction on aryl halide and phenylpropiolic acid. The reaction system is free of a conventional phosphine ligand, so that the environmental pollution is reduced, and the method has good substrate applicability. The target product is easy to separate and purify and high in yield. The method disclosed by the invention is an efficient and safe decarboxylation coupling reaction system and can be applied to constructing Csp-CsP2 bonds.