反应详情

(2R,3R,4R,5R)-2-{6-[(trans-4-Aminocyclohexyl)amino]-2-chloro-9H-purin-9-yl}-5-(2-ethyl-2H-tetrazol-5-yl)tetrahydrofuran-3,4-diyl diacetate (Intermediate 4) (7.9 g) was dissolved in isopropanol (200 ml) and stirred at room temperature under nitrogen. N,N-diisopropylethylamine (10 ml) was added followed by 2,6-dichloro-9-(tetrahydro-2H-pyran-2-yl)-9H-purine (3.92 g). The mixture was stirred at 60° C. under nitrogen for 18 h. 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, dried (MgSO4), and evaporated down in vacuo to give the title compound (10.35 g). Used without purification.

1. stirringThe mixture was stirred at 60° C. under nitrogen for 18 h
2. temperatureto cool to room temperature
3. customevaporated down in vacuo
4. customThe residue was partitioned between ethyl acetate and water
5. customThe organic phase was separated
6. extractionthe aqueous extracted twice with ethyl acetate
7. dry with materialdried (MgSO4)
8. customevaporated down in vacuo