| In view of the allylated thioamide compounds is a good chemical synthesis intermediates and their molecules have important biological activity,in people's production and life have an irreplaceable role,especially in some organic synthesis,are very good synthetic intermediates for the synthesis of sulfur-containing nitrogen heterocyclic compounds and alkaloids.At the same time due to the particularity of their own structure,some allylamine structure have an important biological activity,its also has an important position in the medical profession,naprofen and terbinafine is one of the most typical representative antifungal drugs.Therefore,the synthesis of sulfur-containing allylamine compounds has been the focus of scientific research work,to find a simple,efficient,substrate development and diversification of the new method of synthesis is essential.In this paper,the synthesis of allyl thioamide and its application are reviewed.A series of allylamine derivatives were synthesized by direct allylation of thioamide and primary amines catalyzed by LA,which provided a new idea for the synthesis of allylamine compounds.The main research contents were as follows:1.Al?OTf?3 catalyzed three-component synthesis of allylic thioamide derivatives through a thioamide-paraformaldehyde-alkene condensation reaction.In this reaction,the C-N/C-C bond was successfully constructed without any additives.In addition,we have used a cheaper and richer catalyst,the aluminum?III?salt,to make this method more attractive.2.Al?OTf?3 catalyzed the reaction of primary amine,methyl chloroformate,paraformaldehyde and arylene four component one-pot,to realize the direct allylation of primary amines and the synthesis of a series of allyl amines class compounds.The C-N/C-C/C-C bond was constructed in a pot at the same time,and the operation was simple.This process provides an effective synthesis method for the direct construction of allylamine structural units by primary amines. |
PDF Full Text Request