Preparation method of isatin derivatives

Abstract

The invention discloses a preparation method of isatin derivatives. N-substituted indoline is used as raw materials; tert-butyl hydroperoxide TBHP water solution is used as an oxidizing agent; Cu(OAc)2 is used as a catalyst; the raw materials, the oxidizing agent, the catalyst and the solvent are mixed; then, reaction is performed under the condition of 75 to 95 DEG C for 5 to 30min; the reactionliquid is cooled and is then subjected to washing, extraction separation, drying, solvent removal and purification to obtain the isatin derivatives. The preparation method has the advantages that themethod can further realize the process of directly oxidizing the N-substituted indoline into the isatin derivatives; the reaction operation is simple; the requirement can be met through open opening heating; the reaction time short; the high-yield isatin compounds can be obtained only through 10 minutes; secondly, the catalyst and the oxidizing agent used in the reaction are very cheap; the reaction cost is low; when the specific reaction conditions are used for combination, the yield can reach 88 percent to the highest degree.

Description

technical field [0001] The invention relates to a method for preparing isatin, in particular to a method for preparing isatin derivatives. Background technique [0002] Isatin is widely found in biologically active natural products, pharmaceutical molecules and dye chemistry. Since it is a common multifunctional building block for the synthesis of various useful heterocyclic compounds, the synthetic method of isatin has attracted much attention. Traditional preparation methods often use aniline derivatives as raw materials to prepare isatin derivatives through intramolecular aromatic electrophilic substitution reactions. The reaction routes of these traditional preparation methods are as follows: figure 1 shown. Such methods have significant drawbacks: they usually require relatively harsh reaction conditions, multiple independent reaction steps, difficult-to-obtain substrates, and the use of excessive amounts of acidic or basic catalysts. [0003] Another commonly used m...

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Problems solved by technology

Such methods have significant drawbacks: usually require relatively harsh reaction conditions, multiple independent reaction steps, difficult to obtain substrates, and the use of excess acidic or basic catalysts

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