Formyl-leurosine → methyl (13S,15R,16R,18S)-13-[(1R,9R,10S,11R,12R,19R)-11-acetyloxy-12-ethyl-10-hydroxy-5-methoxy-10-methoxycarbonyl-8-methyl-8,16-diazapentacyclo[10.6.1.01,9.02,7.016,19]nonadeca-2,4,6,13-tetraen-4-yl]-18-ethyl-17-oxa-1,11-diazapentacyclo[13.4.1.04,12.05,10.016,18]icosa-4(12),5,7,9-tetraene-13-carboxylate

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A process for preparing VCR and formylleurosine which comprises oxidizing a tetrahydrofuran solution of the crude dimeric indole-dihydroindole alkaloids obtainable by extraction from the leaves of Vinca rosea in which VLB and leurosine are the predominant alkaloids with an aqueous chromate-sulfuric acid oxidizing solution at a temperature in the range about -80° C. to about -50° C. until substantially all the VLB and leurosine initially present are converted to vincristine and formylleurosine respectively, optionally reformylating any 1-desformyl congeners present, and then separating vincristine and formylleurosine therefrom by chromatography.

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