Functionalized morpholines have attracted much attention due to their potential biological activities. Despite wide importance of morpholine derivatives in drug design of various pharmacological agents, the development of new approaches to their synthesis remains relatively unexplored. Given the low cost and easy availability of N-PROPARGYLAMINES, the synthesis of functionalized morpholines from these versatile building blocks have undergone an explosive growth in recent years. This review provides concise overview on the synthesis of morpholine cores from N-propargyalamines in recent years.

A one-pot, three-component coupling reaction of aldehydes, amines and alkyne (A3-coupling) via C-H activation using perflorinated resinsulphonic acid (Nafion®NR50) as a recyclable and environmentally benign catalyst for the synthesis of propargylamine derivatives is described. This protocol avoids the use of heavy metals, co-catalysts and produces the PROPARGYLAMINES in excellent yields.