New Method For The Synthesis Of Pyrrolidine Compound Within Phosphine Catalyzed Intramolecular Nucleophilic 5-endo-trig Cyclization

Five-membered nitrogen-atom-containing heterocycles constitute one of the most important classes of heterocyclic compounds in the pharmaceutical and agrochemical industries. In particular, pyrrolidine rings have received considerable attention from synthetic community due to their frequent occurrence in nature and wider relevance to numerous biologically active natural products and pharmacologically relevant therapeutic agents.In this work, we described the synthetic method of construct pyrrolidine rings in details.What’s more,a new cyclization for the nucleophilic phosphine catalyzed5-endo-trig cyclizations of N-allylic substituted a-amino nitriles which provides effective synthetic route for the synthesis of functionalized2,4-disubstituted pyrrolidines (N-heterocyclic a-amino nitriles)has been designed.The main contents are as follows:Our work offers a new strategy for achieving amination of N-allylic based on MBH adducts and organic catalysts. In this method, MBH adducts and a-amino nitriles are used as materials to effectively construct polyfunctional a-methylene-β-amino acid derivativecompounds with all-carbon quaternary stereo center. After optimizing the reaction conditions, we explored the influence of solvent and amination of.N-allylic substituent group. This strengthen our comprehension for amination of N-allylic related to the a-amino nitriles. Thus, it paves the way for our future work.Then, the novel cyclization for the nucleophilic phosphine catalyzed5-endo-trig cyclizations of N-allylic substituted a-amino nitriles has been designed. This cyclization provided effective synthetic route for the construction of functionalized2,4-disubstituted pyrrolidines (N-heterocyclic a-amino nitriles).In addition,2,4-disubstituted pyrrolidines was synthesized based on the basic materials through one-pot synthesis method. In this course, some transformations happened in the functional pyrrolidine rings. All these provide potential application value for constructing complex organic molecules.