Cu (Ⅰ) Chiral P/s Ligand Complexes Catalysis Azomethine Ye Lide Of Asymmetric [3 + 2] Cycloaddition Research

1,3-Dipolar cycloaddition reactions are fundamental processes in organic chemistry,1andtheir asymmetric version offers a powerful and reliable synthetic methodology to accessfive-membered heterocyclic rings in regio-and stereocontrolled fashion. Therefore, the1,3-dipolar cycloaddition reaction has very important theoretical significance, and will bewidely applied.Chapter1: Summarized the significance of chiral, chiral compounds synthesis andasymmetric [3+2] cycloaddition reactions in recent years to the development and application.Focusing on the summary [3+2] cycloaddition reactions in the metal precursor, ligands on thechoice of choice, and lists the many scientific research achievements of workers.Chapter2: Cu（Ⅰ） to the chiral P/S ligands complexes catalysis azo armour alkali ylideasymmetric [3+2] cycloaddition reactions were studied. In this section, we focus on thereaction condition are optimized: First of all, in this reaction to explore the effects of bases onasymmetric cycloaddition reaction of azomethine ylide, Separately using the Et₃N i-Pr₂NEt，DBU and K₂CO₃. After test we found to Et₃N alkali additives as the effect is the best. Whenusing DBU, even produced close to extinction of spin effect; And second, we optimize thesolvent, respectively, choose the THF, CH₂Cl₂, toluene and ethyl ether, Found in toluenesolvent for the response of the system not only reaction speed, and by test in toluene solventthat product of ee value, yield and to the enantioselective are higher, so the determined intoluene solvent; At last this paper to design synthesis of six P/S chiral ligands with thepurpose of selection and screening, make sure to use ligands B-1. And finally optimizationout a suitable for the reaction system. Master the above reaction conditions after, we said tothe universality of the substrate to the test and expand to the substrate. Be worth what carry is,in the reaction system with alkali catalyst dosage of additive is very little, just use the1mol%of catalyst and10mol%of alkali additives. And in the substrate universality of theexperiments, made up to99%of the value of more than95:5of the enantioselective, the yieldwas also are achieved85%above, has a broad prospect of application.Chapter3: Target product to a series of test, test results further shows that what weoptimize the reaction conditions was a success, the system shows the comparatively excellentthe corresponding selective （endo: exo>95:5） as well as to the enantioselective, ee%valuecan be as high as99%above.Chapter4: List the reactions of the reaction products of spectra, and a proper explanation,and not just for this paper provides a strong basis in fact, also for the subsequent researchprovides a valuable reference.