6results about How to "Good substrate universality" patented technology

The invention discloses a pyrazolo [5, 1-a] isoindole derivative as well as a synthesis method and application thereof, and belongs to the technical field of organic chemical synthesis. The invention solves the problems of harsh reaction conditions, limited substrate range and the like of continuous multi-step synthesis of a precursor in the existing pyrazolo [5, 1-a] isoindole compound synthesis process. According to the invention, a polarity reversal strategy is adopted, a cyano group is introduced into 1, 5-enyne to change the electronic characteristics of 1, 5-enyne, diazo, olefin and ethynyl benzene are reacted under mild conditions, two rings and three new chemical bonds are constructed through a series of intermolecular [3 + 2] cycloaddition, intramolecular cycloaddition and elimination reactions, and pyrazolo [5, 5-a]-1, 5-a-phenanthrene is efficiently synthesized. According to the present invention, the 1, 1-a] isoindole derivative has characteristics of good synthesis yield, simple operation of the synthesis method, easily available raw materials, good substrate universality and step economy, and provides the effective strategy for the drug design synthesis.

The invention discloses a synthesis method of an aryl phosphine compound as shown in a formula IV, which comprises the following steps: under the irradiation of blue light, reacting a compound as shown in a formula I with a compound as shown in a formula II in an inert atmosphere in an organic solvent in the presence of organic alkali, and then adding S8 to continuously react to obtain the aryl phosphine compound as shown in the formula IV, ar represents a substituted or unsubstituted aryl group, X represents a trifluoromethanesulfonate ion, a hexafluorophosphate ion or a tetrafluoroborate ion, and R1 and R2 each independently represent a substituted or unsubstituted alkyl group, cycloalkyl group or aryl group; and the organic base is selected from any one of N-methyl dicyclohexylamine, triethylamine, tetramethylethylenediamine and N, N-diisopropylethylamine.

The application discloses a method for selectively synthesizing 2-amido quinoline-N-oxide compounds from quinoline-N-oxide compounds, which uses copper hexafluorophosphate tetraacetonitrile and silver acetate as catalysts and isoxazolidinone as nitrogen source, does not need to add expensive ligands, and can obtain the product under mild conditions. The application has the advantages of low cost, mild reaction condition, high selectivity and the like, and avoids the use of noble metals such as rhodium, iridium and palladium. The method is suitable for different substituted quinoline-N-oxide compounds and other polysubstituted isoxazolidinone substrates.

This invention discloses a method for preparing aryl carboxylic acids by reacting aryl thioonium salts with carbon dioxide using a copper compound as a catalyst and diethylzinc as a reducing agent. The aryl thioonium salt substrate is reacted with an organic solvent at room temperature under a carbon dioxide atmosphere at one atmosphere. The product is then acidified and purified to obtain the aryl carboxylic acid. This method uses readily available raw materials, is simple to operate, operates under mild conditions, and exhibits good functional group tolerance and substrate versatility. This method can not only synthesize various simply substituted aryl carboxylic acids but can also be used for the late-stage carboxylation modification of complex drug molecules. The practicality of this method has also been verified on a gram-scale, demonstrating promising prospects for industrial application.

The invention relates to a synthesis method of an alpha-aryl cyclohexanone compound, and belongs to the technical field of photocatalytic organic synthesis, and the synthesis method comprises the following steps: taking aryl diazonium tetrafluoroborate and cyclohexene as raw materials, adding an additive, in the presence of a mixed solvent, under the irradiation of visible light and in the presence of a quantum dot catalyst, carrying out a reaction to obtain the alpha-aryl cyclohexanone compound. Reacting to obtain alpha-aryl cyclohexanone; the invention provides a brand-new synthesis route of the aryl cyclohexanone compound, the cheap aryl diazonium salt and cyclohexene are adopted as raw materials, the alpha-aryl cyclohexanone compound is synthesized through photocatalysis under mild reaction conditions, and the dependence on a noble metal catalyst and harsh reaction conditions in a traditional method is avoided.

The application discloses a method for preparing difluoromethyl compounds by using a photocatalytic LMCT strategy and belongs to the technical field of catalytic synthesis, in particular to a method for preparing difluoromethyl compounds by using a photocatalytic LMCT strategy. The application solves the problems of the existing synthesis method, such as being too complicated, needing pre-activation and a stoichiometric oxidant. The method comprises the following steps: adding olefin compounds, difluoroacetic acid, 2,4,6-triisopropylbenzenethiol and Fe(acac)3 into a solvent to obtain a reaction mixed solution, irradiating the reaction mixed solution by using an LED light source under room temperature and in an inert gas atmosphere, and obtaining difluoromethyl compounds. The application embodies the green reaction and the mild reaction. The method is very simple to operate, various raw materials are commercially available, olefins are easy to prepare, and the reaction can be efficiently realized by using a catalytic amount of a cheap metal catalyst through a one-pot method, so that the method has potential industrial application value. The application can be applied to the field of organic synthesis.