Piperidines, an important class of N‐heterocycles, are very common in naturally occurring bioactive compounds. Recently, functionalized piperidines, specifically, 1,2,6‐triaryl‐4‐arylamino‐piperidine‐3‐ene‐3‐carboxylates have drawn considerable attention due to its diverse pharmacological efficacies that include anti‐cancer, anti‐microbial, anti‐oxidant, anti‐fungal, anti‐inflammatory and acetylcholinesterase (AChE) inhibitory activities. As a result, during the last decade, a number of methods reported for the synthesis of 1,2,6‐triaryl‐4‐arylamino‐piperidine‐3‐ene‐3‐carboxylates via one‐pot pseudo five‐component reactions of aromatic aldehydes, anilines and β‐keto esters under various reaction conditions. The present review deals with the ‘‘up to date” developments on the synthesis of 1,2,6‐triaryl‐4‐arylamino‐piperidine‐3‐ene‐3‐carboxylates reported so far.