Cytidine → Cytarabine

Participants

Reaction Conditions

Reaction Steps

1.0 G of cytidine is dissolved in 20 ml of acetic acid under heating. After cooling, 2.17 g of silicon tetraacetate are added to the solution. The mixture is stirred at 120°C for 5 minutes. The mixture is cooled to room temperature, and 0.6 ml of boron trifluoride-ether complex is added thereto. Then, the mixture is stirred at room temperature for 4 days. After the reaction, the mixture is concentrated under reduced pressure, and the residue is treated in the same manner as described in Example 3. 0.5 g of 1-β-D-arabinofuranosyl cytosine is thereby obtained. Yield: 50 % M.p. 213°-214°C (decomp.) (recrystallized from 50 % ethanol)

Provenance & Evidence