A NEW PROCESS OF THE SYNTHESIS OF 3',4'-ANHYDROVINBLASTINE, VINBLASTINE AND VINCRISTINE

摘要

The present application relates to a method forproducing dimer alkaloid compounds especially of the Catharanthus(Vinca) alkaloid groups and, in particular, for producing theanti-viral, anti-leukemic (antineoplastic) compounds vincristineand vinblastine. Use of selected 1,4-dihydropyridine compoundsfor the 1,4-reduction of an iminium intermediate to an enamineresults in significant increase in the yield of the enamine.Parameters for the oxidative transformation of enamine to theiminium intermediates and subsequent reduction of the iminiumintermediates to vinblastine and leurosidine are disclosed. Theoverall process, conducted in a one-pot operation, producingvinblastine, leurosidine and 3',4'-dehydrovinblastine isdescribed.