Ammonia → HCID 131734443, compound

Participants

Reaction Steps

In a round bottom flask, fumaric acid salt of ((R)-((1-(6-amino-9H-purin-9-yl)propan-2-yloxy)methyl)(phenoxy)phosphoryloxy)methyl pivalate (50 g), water (500 ml) and liquid ammonia (50 ml) at 23-25° C. The reaction mass was stirred for 30 minutes and extracted with dichloromethane (500 ml). The organic layer was collected and distilled under vacuum. To the residue, 135 ml water and 27 ml acetonitrile was added. The contents were stirred at 23-25° C. for 15 minutes. L-tartaric acid (4.25 g) was added and stirred at 55-60° C. The material was filtered, washed with acetonitrile and dried at 40-45° C. to obtain ((R)—(((R)-1-(6-amino-9H-purin-9-yl)propan-2-yloxy)methyl)(phenoxy)phosphoryloxy)methyl pivalate L-tartarate. (Yield—10 g, 80% diastereomeric purity). The solid was purified with water and acetonitrile to obtain ((R)—(((R)-1-(6-amino-9H-purin-9-yl)propan-2-yloxy)methyl)(phenoxy)phosphoryloxy)methyl pivalate L-tartarate (Yield—7 g, 95% diastereomeric purity).

Provenance & Evidence