De novo incorporation of N-formylated aminols as strategic substrates in legendary Ugi cyclization. Lactamization of N-formido alkanols is accomplished by a novel Parikh–Doering oxidation–dehydration–Ugi cyclization cascade leading to the formation of lactams up to eight carbons (ring size; n= 1–4) in moderate yields using formidoaminol, substituted aniline, and aliphatic/aromatic carboxylic acid derivatives as starting materials.