The Investingation Of Synthetic Methods Of Bis(Indolyl)Methanes And Isoxazolines By Grinding Process

Ball-grinding solid state reaction has many advantages, such as process simply; react quickly; environmentally friendly and so on. This method has attracted the researcher’s attention in recent years. This thesis main discussed the synthesis of three drug intermediates by grinding method, these three substances are β-indolone, bis(indolyl)methanes and isoxazolines, respectively. And from it, we discussed the application of grinding method in organic reaction, and decided the optimal scheme of some synthetic drug intermediatesChapter One The research progress of Bis(indolyl)methanesThis chapter describes the features and promising applications of grinding method. And gives a simply review on the bioactivity of Bis(indolyl)methanes. In the field of drug synthesis, it was been proved that this materials has large developmental potentiality. At the same time, we reviewed the recent developments of the indole and bis(indolyl)methanes. This research afforded a theoretic basis for farther research and industry application.Chapter Two Synthesis of Bis(indolyl)methanes catalyzed by sulfamic acid through mechanochemical processBasis on the experiments, a general mechanochemical route to synthesis bis(indolyl)methanes has been established for a bound range of aldehydes with indole via a simple mortar-pestle grinding method. The bis(indolyl)methane derivatives are obtained in superior yields under room temperature condition, within a short time, and sulfamic acid is found to efficiently catalyze the reaction, the catalyst could be recovered by simple filtration from the reaction mixture without further treatment and reused several times with consistent catalytic activity. For optimal results, the amount of catalyst has been investigated. And the proposed reaction mechanism has also been deduced as the same time.Chapter Three synthesis of β-indoloneTo adequately reap the medicinal value of indole, with solid sulfamic acid as catalyst we have designed two synthetic routes of β-indolone acetate from indole and chalcone. Firstly chalcone have been successfully synthesized, meanwhile the grinding reaction conditions and methods were studied in detail. Although it failed to meet the target product, but we synthesized Bis(indolyl)methanes by grinding method. it provides us a new method and idea for the next work.Chapter Four The grinding synthesis reaction of chalcones with hydroxylamine hydrochloride under the solvent assisted conditionIn this chapter, we discussed the grinding synthesis reaction of chalcone with hydroxylamine hydrochloride under room temperature via base catalysis. As a consequence, a new material has been found. The kind of catalyst has been investigated, and the optimal experimental conditions also were determined. At last, some existing problems of grinding were analyzed in the end of experiment.Finally, we make a conclusion to the article, discussed the used of grinding method and nonmetal catalyst. Some spectra are listed...