Stavudine → Stavudine DMA

Participants

Reaction Conditions

Reaction Steps

Crude slightly beige Stavudine (17.25 g, 96.02% pure, 0.0739 mole) was combined with N,N-dimethylacetamide (25.91 g, 1.5 parts) and isopropanol (52 mL, 3 volumes) and heated to 79° C. when all solids dissolved. The cloudy mixture was filtered through dicalite and washed with isopropanol (12.5 mL). The filtrate was initially concentrated at atmospheric pressure and then a slight vacuum was applied so that the distillation occurred at 60-70° C. It was estimated that about 1.7 g of isopropanol remained. The solution was cooled, filtered, washed and dried to give 17.30 g of Stavudine-DMA solvate (0.0556 mol, 75.2%) with a chromatographic purity of 99.59%.

Provenance & Evidence