碱促进的无催化剂、无溶剂条件下三取代吡唑衍生物的绿色合成-化学专业论文.docxVIP

内蒙古大学硕士学位论文基卤化物的偶联反应进行了初步研究，虽经过大量实验，但目前仍未 内蒙古大学硕士学位论文 基卤化物的偶联反应进行了初步研究，虽经过大量实验，但目前仍未 获得令人满意的结果，该工作我们课题组仍在进行中。 关键词：无催化剂；无溶剂；a,13．炔基腙；三取代吡唑；绿色化学 万方数据 内蒙古大学硕士学位论文BASE．PRoMoTED 内蒙古大学硕士学位论文 BASE．PRoMoTED ECo．FRIENDI』Y SYNTHESIS 0F TRISUBSTITUTED PYRAZoLES UNDER METAL．AND SoLVENT_．FREE CoNDITIoN ABSTRACT Pyrazole is one of the important N-heterocycle broadly found in many natural products and pharmaceutically active molecules and frequently used as useful ligands for metal catalyzed cross-coupling reactions in organic synthesis，biological medicine and material science． Several methods have been reported for the synthesis of substituted pyrazoles by literatures．However,the use of hazardous transAion metals， harsh reaction conditions，tedious workup procedures as well as poor regioselectivity are the main drawbacks of many of these methods．To overcome these difficulties，the development of more convenient and efficient synthetic methodologies is still desirable． This paper mainly described a simple，efficient and green method for the synthesis of trisubstituted pyrazoles from 伐，p—alkynic N-tosylhy’drazones under metal-and solvent-free conditions．Only‘Pr2NH was required as the promotor here and the reaction Can be easily performed at room temperature and also in gram scale．It was found that lll 万方数据 内蒙古大学硕士学位论文the 内蒙古大学硕士学位论文 the reaction proceeded smoothly over a wide range of substrates and afforded the corresponding pyrazoles in higll yields．This approach displayed some advantages compared to the conventional methods，such as shorter reaction time，mild reaction temperature，high isolated yields as well as regioselectivities，and the ease of purification of the products．In addition，we proposed a possible mechanism of this transformation． On the other hand，we have investigated the Pd-catalyzed coupling reactions of a，13．alkynic hydrazones with benzyl halides．Although a lot of experiments have been performed，the satisfactory results has not yet obtained．Further exploitation is cur