Dialkyl phosphite as highly selective N-alkylating agent using p-toluene sulphonic acid as catalyst

Abstract

The presence of carbon–nitrogen bond is widely found in different useful synthetic intermediates, organic solvents, dyes, fine chemicals, biologically relevant molecules (e.g. amino acids, DNA and RNA bases etc), pharmaceuticals, agrochemicals, and catalysts.1 Amines and their derivatives are prevalent functionalities in various natural products and unnatural synthetic targets. Due to its unique biological properties, the amine moiety has played a central role in chemotherapeutics of numerous diseases.2 Polyamines and peptidomimetics have constituted some of the most popular targets in recent combinatorial approaches in drug development.3 Because of such versatile importance of amines, development of versatile and efficient methods for the synthesis of amines has attracted much attention and is still occupying an active area of research