2-(Methylamino)ethanol → 2-(4-(4-Cyano-2-(methylsulfonyl)phenyl)-2,5-dioxo-1-(3-(trifluoromethyl)phenyl)-6,7-dihydro-1H-cyclopenta[d]pyrimidin-3(2H,4H,5H)-yl)-N-(2-hydroxyethyl)-N-methyl-acetamide

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Reaction Steps

A solution of 2-(4-(4-cyano-2-(methylsulfonyl)phenyl)-2,5-dioxo-1-(3-(trifluoromethyl)-phenyl)-6,7-dihydro-1H-cyclopenta[d]pyrimidin-3(2H,4H,5H)-yl)acetic acid (example 19, 23 mg, 43 μmol) and triethylamine (18 μL, 0.13 mmol) in N,N-dimethylformamide (1.0 mL) is stirred at room temperature for 5 min and treated with N,N,N′,N′-tetramethyl-0-(benzotriazol-1-yl)uronium tetrafluoroborate (13 mg, 43 μmol). After 5 min, 2-(methyl-amino)ethanol (10 μL, 0.13 mmol) is added. The mixture is stirred at room temperature for 3 h and purified by reversed phase HPLC (Waters Xbridge™-C18, gradient of acetonitrile in water, 0.1% NH3). Yield: 15 mg; ESI mass spectrum [M+H]+=591; Retention time HPLC: 0.89 min (Z011_S03).

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