Preparation method of cyclopropane derivative

Abstract

The invention belongs to the technical field of organic chemical synthesis, and discloses a preparation method of a cyclopropane derivative, which comprises the following steps: 1) adding a drying agent into a pyrazoline compound, mixing, standing, separating liquid, and collecting supernatant liquid to obtain a dried pyrazoline compound; 2) adding a catalyst into the dried pyrazoline compound, and mixing to obtain a reaction solution; 3) heating the reaction liquid until the temperature of the reaction liquid reaches 180-190 DEG C, and starting to collect condensate generated by distillation; 4) continuously heating the reaction liquid to 200-210 DEG C, and preserving heat until no condensate is generated; and 5) continuously heating the reaction liquid to 230-240 DEG C, preserving heat until no condensate is generated, and collecting the condensate, namely the target product. The preparation method disclosed by the invention is simple in process condition, high in reaction yield, less in three wastes generated in the preparation process and suitable for industrial amplification, and the obtained target product can meet the use requirements of the cyclopropane derivative as a medical intermediate or used for preparing a spaceflight propellant.

Description

technical field [0001] The invention belongs to the technical field of organic chemical synthesis, and in particular relates to a preparation method of cyclopropane derivatives. Background technique [0002] Cyclopropane derivatives have high strain energy due to their three-membered strained ring structure. One of its main functions is to be used in the preparation of aerospace propellants, which can be used as fuel components of rocket propellants and help to improve the specific impulse performance of propellants. In addition, cyclopropane derivatives are also widely used in the field of medicine. Research data show that cyclopropane derivatives can enhance the efficacy of drugs, reduce off-target effects, improve metabolic stability, limit the conformation of polypeptides, and slow down their hydrolysis. At present, cyclopropane derivative drug components are common in people's daily medication, and ciprofloxacin is an example. Therefore, the research on the synthesis...

AI Technical Summary

Problems solved by technology

In the above-mentioned reaction process, iodine zinc reagent, transition metal catalyst and corresponding ligand, Grignard reagent or diazonium reagent are usually used. The operating conditions of these reagents are usually harsh and require anhydrous and oxygen-free conditions. The control requirements are extremely high, and it is difficult to apply to the industrial production of cyclopropane derivatives

Especially like diazo reagent, which is flammable and explosive, and its application in industrial production will lead to greater safety hazards

On the other hand, the reaction yield of preparing cyclopropane derivatives by the above reaction is usually only less than 90%, and there is a waste of raw materials in industrial production.

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