Study On Annulations Of α-Amide Ketene Dithioacetals With Dicarboxylic Acid Dichlorides And Aplications

α-oxo Ketene dithioacetals are siginificant organic synthesis intermediates, thefunctional groups are dense in the molecular, α-oxo Ketene dithioacetals have aplurality of reactive, it can occur many types of cyclization reactions. For example [3+2][2]、[3+1+1][3]、[3+3][4]、[4+2][5]、[5+1][6]、[7+1][7]cyclization. Thus,it has a very wide range of applications to construct the carbo-or heterocylic structureand cyclic biological activity compounds.In the α-amide ketene dithioacetals molecule, β-double alkylthio and α-carbonylwith the push-pull electronic effect of the C=C is highly polarized, therefore, theα-carbon electron cloud density is greatly increased, making α-amide ketenedithioacetals is easily react with a series of dear electric reagents. Then, the nitrogenatom of α-amide ketene dithioacetals with dear nuclear make it became a veryimportant class of1,3-binucleophilic fragments in organic synthesis.Cyclization reaction is a siginificant research contents in the field of organicsynthesis research. Exploring a novel α-functionalized cyclization reaction has beenone of the main research contents of our research group. This thesis explores this fieldnewly and the main content includes the following:1. To achieve the ketene dithioacetals as1,3-binucleophilic fragments in thenovel cyclization reaction. Developing the [3+n] cycloaddition reaction of α-amideketene dithioacetals and di-carboxylic acid dichlorides, in a catalyst free conditions. Aseries of potentially biologically active nitrogen heterocyclic compounds weresynthesized. Consequently, to establish a new methord for the synthesis of nitrogenheterocyles from readily available starting materials.2. To explore the further application of nitrogen heterocyclic productsPyrrolidinetriones and Piperidinetriones. To develop the cycloaddition reaction of itand the amidine compounds. Finally, a series of pyrimidine derivatives is synthetizedeffectively.3. The synthesis method has mild conditions and in good to excellent yields.The heterocyclic products were confirmed by1H NMR and high resolution MassSpectrometry characterization.Key words: α-Amide Ketene dithioacetals;1,3-Binucleophilic Fragments;[3+n]...