Aldehyde-Induced Metal-Free Decarboxylation Of ?-Amino Acids To Synthesize N-Alkyl-?-Alkenyl Cyclic Amines With High Stereoselectivity

Nitrogen-containing heterocyclic compounds have an invaluable value in both biological and non-biological fields.The synthesis of N-containing heterocyclic compounds with an efficient,simple,and safe method has been a hot spot for organic chemists.In contract to the dependence of transition metal and complex organic ligands on traditional coupling reaction.In this paper,a one-pot difunctionalizative reaction has been developed for the aldehyde-induced metal-free decarboxylation of a-amino acids to synthesize N-alkyl-?-alkenyl cyclic amines with high stereoselectivity.Concrete research content is as follows:The first chapter introduced the general situation of coupling reaction and the development course of oxidative decarboxylation coupling reaction as well as the current researcher progress of predecessors' research in this field.In addition,some problem were described in detail,which provided the theoretical support for putting forward the research.In the second chapter,firstly,the possible biological activity of the product is briefly introduced.Then,it is necessary to confirm the necessity and feasibility of the experimental study.The optimum reaction condition were obtained by a large number of experiments.Then,the reaction substrate is extended.At last,we also speculate on the possible mechanisms of the reaction and provide arguments for the conclusion.In the third chapter a large number of experiments were carried out under the optimum reaction conditions to obtain compounds with potential drug activity.All the compounds were confirmed by 1H-NMR?13C-NMR and mass spectra.In summary,we have successfully developed the aldehyde-induced decarboxylation of a-amino acids without any metallic reagents.In the process,metal catalyst and toxic ligands were not used,which is difficult to achieve for traditional chemical methods.From a synthetic point of view,it complements the other catalytic methods used for C(2)-fuctionalization of a-amino acids.The synthesis of this method in the industry and the more accurate synthesis mechanism has yet to be further explored.