3results about How to "Good functional group tolerance" patented technology

The invention discloses a method for preparing a beta-trifluoromethyl substituted enamine compound from trifluoromethyl thianthrene salt, which comprises the following steps: by taking the trifluoromethyl thianthrene salt as a trifluoromethyl source, synthesizing enamine ester or 4-amino coumarin from a first component amine and an electron-deficient terminal alkyne compound; and synthesizing the beta-trifluoromethyl substituted enamine compound from the first component and a second component trifluoromethyl thianthrene salt in two steps. According to the method for preparing the beta-trifluoromethyl substituted enamine compound through two steps, the synthesis method is mild in reaction condition, free of inert gas protection, capable of being carried out at the room temperature in the air atmosphere, good in functional group tolerance and wide in substrate universality, the separation and purification process is easy to operate, and the method is suitable for industrial production. And a target product with high site selectivity can be generated at a good to excellent yield. According to the synthesis strategy, the reaction steps are effectively shortened, the atom economy is greatly improved, meanwhile, the cost required by the preparation process is remarkably reduced, and large-scale industrial production can be achieved.

The invention relates to the fields of medicine, organic chemical industry and fine chemical industry, and particularly discloses a method for synthesizing an isoindolinone compound through palladium catalysis. According to the method, oxamide-protected benzylamine and ethyl glyoxylate are taken as raw materials, and the isoindolinone compound is synthesized in the presence of a palladium catalyst, an oxidizing agent and an additive. The reaction conditions are as follows: the reaction lasts for 24-36 hours under the heating condition of 100-120 DEG C; trifluorotoluene, toluene, chlorobenzene and acetonitrile are used as reaction solvents; di-tert-butyl peroxide, cumyl hydroperoxide, tert-butyl hydroperoxide and tert-butyl peroxybenzoate are used as oxidizing agents; and sodium persulfate and potassium persulfate are used as additives. And a series of substituted isoindolinone compounds can be obtained at high yield after simple post-treatment in the reaction.

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.