Macrocycles are circular molecules with 12 or more atoms that bind to large, flat or flexible protein surfaces inaccessible to conventional small drugs[1][2]. Their three-dimensional structure acts as a ready-made key for specific bioactive sites[1]. Traditional methods for the synthesis of macrocyclic compounds require multi-step processes and it is difficult to control the resulting 3D structure due to the high energy barrier[1]. Rackl et al. published a study where a bifunctional peptide organocatalyst directs the ends of a linear precursor to form 12- to 18-membered rings with a predictable 3D structure[1][2]. The catalyst prefers an intramolecular reaction to an intermolecular one and precisely controls the stereochemistry of newly formed stereogenic centers[2]. The method produces diverse macrocyclic lactones and lactams from achiral linear precursors and even determines the stereochemistry of the chiral precursor[2]. This synthesis was demonstrated by the synthesis of the core of the natural product robotnikinin[2]. The approach avoids difficult multi-step syntheses and can speed up the discovery of new drugs[1].