Efficient Synthesis of β-Lactam-Containing α-Aminophosphonates Using Fumaric Acid as Mild Catalyst

Abstract

A short and efficient protocol for the synthesis of novel α-aminophosphonate esters containing β-lactam moiety is described. Inexpensive and mild catalyst such as fumaric acid was used for the synthesis of α-aminophosphonate esters by reacting N-(4-methoxyphenyl)-2-(substituted) propiolactam-3-carbaldehyde with amine and triethylphosphite in acetonitrile at reflux. α-aminophosphonate esters containing β-lactam hybrids were obtained in good yield and purity.<br /><br /><br />A short and efficient protocol for the synthesis of novel α-aminophosphonate esters containing β-lactam moiety is described. Inexpensive and mild catalyst such as fumaric acid was used for the synthesis of α-aminophosphonate esters by reacting N-(4-methoxyphenyl)-2-(substituted) propiolactam-3-carbaldehyde with amine and triethylphosphite in acetonitrile at reflux. α-aminophosphonate esters containing β-lactam hybrids were obtained in good yield and purity.