Researchs On The Synthesis And Application Of 1,2,3-Triazoles Via Cu(Ⅰ)-catalyzed

The 1,2,3-triazoles, as important heterocyclic compounds, hase been known formore than one hundred years. Due to their unique chemical and structural properties,they have received much attention over the past decades and found wide applicationin organic chemistry, organometallic chemistry, medicinal chemistry and materialscience. We are interesting in the synthesis and the application of 1,2,3-triazoles inthis paper, which including the following:In the first chapter, we reviewed mainly the development of Huisgen's 1,3-dipolar[3+2]-cycloaddition from organoazides and alkynes or alkenes to synthize1,2,3-triazoles in recent years. Since Cu(I)-catalyzed Huisgen reaction has reported asan useful process to connect diverse building blocks of organoazides and alkynes, thereaction has made great progress in the synthesis of 1,4-disubstituted and1,4,5-trisubstituted 1,2,3-triazol-synthesis researchs. Compared with traditionalHuisgen reaction, Cu(I)-catalyzed Huisgen reaction are mild-conditions, high yieldand high regioselectivity. At the same time, others transitional-metals were used in thesynthesis of triazoles.In chapterâ…¡, a summary of 1-monosubstituded-1,2,3-triazole was introducedbriefly. Against previous researches, Cu(I)-catalyzed Huisgen reaction wasimplemented from organoazides and acetylene gas under normal pressure at roomtemperature. The screening and optimization of the experimental conditions showedthat CuI/Et₃N in catalytic amount and dimethyl sulfoxide (DMSO) is essencial to givethe good results.The third chapter is devoted to the combination of the Cu(I)-catalyzed Huisgenreaction, organocatalysts and ionic-liquid supported synthesis. From Cu(I)-catalyzedHuisgen reaction, an ionic-liquid-supported organocatalyst was synthesizedsuccessfully. The ionic-liquid-supported organocatalyst shown the good catalyticalactivity in the direct Michael addition of ketone withβ-nitroalkene. The ionic-liquid-supported organocatalyst could recyclization and reuse facilely, and infour times of reuses, no significant loss of catalytic activity was found.