Metal-free Catalytic Synthesis Of Polysubstituted Oxazoles And A Study On Synthesis Of Pinaeolone

The multifunctional oxazoles of five-membered heterocycles are one of the important privileged scaffolds existing widely in a broad array of natural compounds and are generally considered as an indispensable chemical block in organic synthesis.Pharmacologically synthesized molecules with attractive biological activities have important applications in medicine and have always been one of the research focuses of many chemical workers.We have proposed a new method for the synthesis of multi-substituted oxazoles based on the principle of high efficiency,simplicity,economy,and environmental protection.This paper refers to the scheme of preparation of oxazole compounds in the past 20 years,and reporte a new scheme for the synthesis of polysubstituted oxazole compounds by metal-free catalysis.This article mainly includes the following three parts:Chapter ? Multi-Substituted Oxazole Compounds are a very important class of five-membered nitrogen-containing heterocyclic compounds with good biological activity.Therefore,they are widely used in medicine,organic synthesis,and materials.This paper describes in detail the application and synthesis of multi-substituted oxazole compounds.Chapter ? 2,5-Substituted oxazole compounds were usually acquired by direct reaction of Phenylacetylene and Benzylamine by I₂/TsOH in solvent DMSO.This is a simple and efficient method for the synthesis of 2,5-substituted oxazole compounds by iodine catalyzed phenylacetylene and benzylamine via[3+2]cycloaddition.This method has the advantages of using an inexpensive catalyst,no ligand,high yield,mild reaction conditions,and excellent product selectivity.Importantly,this method provides a novel synthetic route for the synthesis of2,5-oxazoles.Chapter ? Pinacolne,because of the special functional group carbonyl group and its special structure,has broad application prospects in organic fine chemicals.This paper introduced in detail the optimization of pinacolne with chloro-tert-pentane supplied by Nantong as the raw material.The optimization of the pinacolne synthesis parameters can guide industrial production.