Bleomycin is an important antibiotic for the treatment of cancer. Now the completion of the total synthesis of the aglycon 1 from bleomycin A2, the major component of bleomycin, has been achieved. The decisive steps are the construction of the pyrimidine part by an inverse‐electron‐demand Diels–Alder reaction and the diastereoselective addition of a stannous enolate to an imine group. (Figure Presented.) Copyright © 1993 by VCH Verlagsgesellschaft mbH, Germany