A new process of the synthesis of 3',4'-anhydrovinblastine,...

C - Chemistry – Metallurgy – 07 – D

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260/237.3

C07D 519/04 (2006.01)

Patent

CA 1341262

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

543832

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