反应详情

To a solution of 4-[4-(2,6-Dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1H-purin-8-yl)-phenoxymethyl]-pyrrolidine-2-carboxylic acid methyl ester (50 mg, 0.106 mmol) and TEA (32 mg, 0.319 mmol) in DCM (5 ml), 3-trifluoro methyl benzyl bromide (30 mg, 0.127 mmol) was added at 0° C. Reaction mixture was stirred at room temperature for 4 hr. Water was added into it and extracted with DCM. The organic layer was washed with brine, dried over Na2SO4, filtered and concentrated under vacuum to offer 4-[4-(2,6-Dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1H-purin-8-yl)-phenoxymethyl]-1-(3-trifluoromethyl-benzyl)-pyrrolidine-2-carboxylic acid methyl ester as an off white solid (25 mg, 37%).

1. customReaction mixture
2. extractionextracted with DCM
3. washThe organic layer was washed with brine
4. dry with materialdried over Na2SO4
5. filtrationfiltered
6. concentrationconcentrated under vacuum