Synthesis of Vinblastine Derivatives

The bisindole alkaloids of the Madagascan periwinkle Catharanthus Roseus vincristine 1 and vinblastine 2 are widely used clinically in the chemotherapy of cancer. Many efforts were made to synthesize more efficient new derivatives having less side effects than vinblastine 2. New anhydrovinblastine derivatives were obtained by the ferric chloride mediated coupling reaction of catharanthine and vindoline and their derivatives. The nitro- dinitro-, amino- and hydroxymethyl analogues of the alkaloids 1, 2 and 3 showed promising antitumor activity.