CuI.Catalyzed Synthesis Of Pyrimidin-ones Functionalized1,2,3-triazole Derivatives And I₂Catalyzed Synthesis Of Quinoline And Benzoxazine Derivatives

1,2,3-triazoles are important five-membered heterocyclic compounds, most ofthem have biological activity and unique chemical properties. They are widely used inorganic chemistry, organometallic chemistry and pharmaceutical chemistry. Thiscompound can be obtained by Huisgen cycloaddition. Usually,1,2,3-triazoles weresysnthesized by the Cu(I)-catalyzed cycloaddition of alkynes with azides. Researcheson1,2,3-triazoles are concentrated on synthetic methodology and its applications indrug.Based on the summarized the synthesis and research progress of C2-substituted-pyrimidines and1,2,3-triazoles, the thesis have explored the method of synthesizingC2-substituted pyrimidines-1,2,3-triazoles through pyrimidines functionalizedpropyne. The synthesis method is operated simply with good regioselectivity andmoderate yields. We have also explored the I2-catalyzed one pot reaction of N-arylbenzamides, paraformaldehyde with styrene that leads to new quinolines andbenzoxazines by different conditions. The main contents are as follows：1. A mild and rapid procedure to the synthesis of2-hydroxypyrmidines wasdeveloped via sequential functionalization of easily available Biginelli3,4-dihydropyrimidine-2(1H)-ones via oxidation, followed by cross-coupling reactionwith propargyl alcohol under Mitsunobu conditions.2-hydroxypyrmidines were alsoprepared via sequential functionalization of easily available Biginelli3,4-dihydropyrimidine-2(1H)-ones via oxidation, esterification, followed by cross-coupling reaction of pyrimidin-2-yl sulfonates with propargyl alcohol.The structuresof componds were confirmed by1H NMR,13C NMR.2. Pyrimidine functionalized1,2,3-triazoles were synthesized by CuI-catalyzedone pot three components of C2-propargyloxy pyrimidines, NaN3and haloalkane. Thestructures of componds were confirmed by1H NMR,13C NMR. The method isoperated simply, and the reaction is rapid and it is not necessary to separateintermediate of organic azide.3. We explored I2-catalyzed multicomponent reaction of aryl amide,paraformaldehyde and styrene. The reaction leads to benzoxazines, quinolines and formylation products. The the structures of componds were confirmed by1H NMR,13C NMR...