Abstractβ‐Carboline ring is widely distributed in nature and several β‐carboline alkaloids were extracted from marine creatures, bacteria, fungi, food stuffs, plants, and mammals. Synthetic β‐carbolines derivatives were reported to exhibit various biological activities. This review highlighted the recent progress achieved in the last decade in the Pictet‐Spengler synthesis of β‐carboline derivatives with a special focus on the green methods and green catalysts used for the synthesis.