Acetaldehyde → 3-Cyclopropylmethyl-8-[4-(ethyl-amino)-benzyl]-1-(2-fluorobenzyl)-3,7-dihydro-purine-2,6-dione

Beteiligte Stoffe

Reaktionsschritte

To a suspension of 10% palladium on carbon (0.10 g) in tetrahydrofuran (50 mL) was added 3-cyclopropylmethyl-8-[4-aminobenzyl]-1-(2-fluorobenzyl)-3,7-dihydro-purine-2,6-dione (prepared as described in example 64, step 1) (0.21 g, 0.50 mmol) and acetaldehyde (72.6 μL, 1.3 mmol). The mixture was shaken under an atmosphere of hydrogen at 1 atmosphere pressure and ambient temperature for 3 days. The catalyst was removed by filtration through celite, washing the filter pad through with tetrahydrofuran and methanol. The combined filtrate was concentrated in vacuo and the residue purified by chromatography using silica eluted with 1:1 hexanes/ethyl acetate. Concentration of the appropriate fractions gave the product as a colorless solid (0.14 g, 62%). MS, m/z(M+H)=553.

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