Isopropanol → HCID 178463187, compound

Participants

Reaction Conditions

Reaction Steps

(2R,3R,4R,5R)-2-(2,6-Dichloro-9H-purin-9-yl)-5-(2-ethyl-2H-tetrazol-5-yl)tetrahydrofuran-3,4-diyl diacetate (10 g) (ref WO98/28319A1) was suspended in isopropanol (100 ml). 1,1-Dimethylethyl(trans-4-aminocyclohexyl)carbamate (4.56 g) and N,N-diisopropylethylamine (5.6 ml) were added and the mixture heated at 65° C. under nitrogen overnight. The reaction mixture was allowed to cool to room temperature and evaporated down in vacuo. The residue was partitioned between ethyl acetate and water. The organic phase was separated and the aqueous extracted twice with ethyl acetate. The organic phases were combined, washed with water, dried (Na2SO4), and evaporated down in vacuo, dried under high vacuum overnight, to give the title compound, 12.49 g.

Provenance & Evidence