Jump to main content
Jump to site search


Ru-catalyzed cascade reaction of α,ω-alkynoic acids and arylethylamines towards the synthesis of aryl-fused heterocycles

Abstract

A simple, efficient, and mild method for the preparation of aryl-fused heterocycles has been developed using α,ω-alkynoic acids and arylethylamines. In the present method, one of Grubbs’ Ruthenium carbenes is able to catalyze the formation of exocyclic enol lactones from α,ω-alkynoic acids, which subsequently undergo aminolysis and N-acyl iminium ion formation/cyclization with arylethylamines in the presence of TFA, affording one kind of “drug-prejudiced” scaffolds. Demonstrated with high functional group tolerance, this new cascade reaction endow the Grubbs’ Ruthenium carbene a new synthetic utility beyond routine olefin metathesis.

Back to tab navigation

Supplementary files

Article information


Submitted
16 Nov 2019
Accepted
10 Jan 2020
First published
13 Jan 2020

Org. Chem. Front., 2020, Accepted Manuscript
Article type
Research Article

Ru-catalyzed cascade reaction of α,ω-alkynoic acids and arylethylamines towards the synthesis of aryl-fused heterocycles

Y. Zheng, J. Liu and X. Lei, Org. Chem. Front., 2020, Accepted Manuscript , DOI: 10.1039/C9QO01375J

Social activity

Search articles by author

Spotlight

Advertisements