反应详情

4-Trifluoromethyl-phenyl isocyanide (0.018 g, 0.096 mmol) was added to a solution of 3-(3-Amino-benzyl)-2-(2-amino-pyrimidin-4-yl)-1-methyl-4-oxo-1,4,6,7-tetrahydro-pyrrolo[3,2-c]pyridine-5-carboxylic acid tert-butyl ester (0.039 g, 0.088 mmol) (prepared as described in Example 6) in DCM (2.0 ml) and the reaction mixture was stirred at room temperature for 3 h, under an argon atmosphere. MTBE (5.0 ml) was added to the reaction mixture and the organic layer was washed with purite water (1×5.0 ml), brine (1×5.0 ml), dried over Na2SO4. The filtrate was dried under vacuum and the crude was purified by reverse phase chromatography, affording 2-(2-Amino-pyrimidin-4-yl)-1-methyl-4-oxo-3-{3-[3-(4-trifluoromethyl-phenyl)-ureido]-benzyl}-1,4,6,7-tetrahydro-pyrrolo[3,2-c]pyridine-5-carboxylic acid tert-butyl ester (0.051 g, 0.080 mmol, 93%).

1. washthe organic layer was washed with purite water (1×5.0 ml), brine (1×5.0 ml)
2. dry with materialdried over Na2SO4
3. customThe filtrate was dried under vacuum
4. customthe crude was purified by reverse phase chromatography