Acetic Acid → 2-(((3aR,4S,6R,6aS)-6-(7-Chloro-5-(propylthio)-3H-1,2,3-triazolo(4,5-d)pyrimidin-3-yl)tetrahydro-2,2-dimethyl-4H-cyclopenta-1,3-dioxol-4-yl)oxy)ethanol

Participants

Reaction Steps

To 2-[((3 aR,4S,6R,6aS)-6-{[5-Amino-6-chloro-2-(propylthio)pyrimidin-4-yl]amino}-2,2-dimethyltetrahydro-3 aH-cyclopenta[d][1,3]dioxol-4-yl)oxy]ethanol (180 kg) in toluene (749 kg) and acetic acid (153 kg) were added sodium nitrite (33.2 kg) in water (88 kg) charged with a rate that kept the temperature of the reaction ≦30° C. After the conversion criterion was reached (>99%) potassium carbonate (176 kg) in water (360 kg) was added to the reaction solution whereafter the water layer was separated off and the organic-layer was used in the next step.

Provenance & Evidence