反应详情

A mixture of 4-[(1,1-dimethylethyl)oxy]benzoic acid (Apin chemicals) (117 mg, 0.603 mmol), HATU (232 mg, 0.610 mmol), Hunig's base (0.263 mL, 1.506 mmol) in N,N-Dimethylformamide (DMF) (1 ml) was stirred for 1 hr before the addition of N-hydroxy-5-isoquinolinecarboximidamide (D1; 94 mg, 0.502 mmol) in N,N-dimethylformamide (DMF) (1 ml). The reaction was left to stir at room temperature for 2 hrs and then heated to 120° C. for 2 hr in the microwave. The reaction mixture was concentrated in vacuo and purified by preparative HPLC (Waters Sunfire C18 column, eluting with solvents A/B (A: Water+0.1% Formic acid, B: MeCN+0.1% Formic acid)) to give the title compound (31.5 mg)

1. waitThe reaction was left
2. temperatureheated to 120° C. for 2 hr in the microwave
3. concentrationThe reaction mixture was concentrated in vacuo
4. custompurified by preparative HPLC (Waters Sunfire C18 column
5. washeluting with solvents A/B (A: Water+0.1% Formic acid, B