Abstract β‐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.