反应详情

A mixture of 3,5-dichloro-4-(propyloxy)benzoic acid, (Maybridge) (150 mg, 0.603 mmol), HATU (232 mg, 0.610 mmol), Hunig's base (0.263 mL, 1.506 mmol) and 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 mixture was left to stir for 2 hrs at room temperature and then heated to 120° C. for 2 hr in a microwave. The cooled reaction mixture was concentrated in vacuo and the residue purified by Mass Directed Preparative HPLC (Supelcosil ABZ+Plus column, eluting with solvents A/B (A: Water+0.1% Formic acid, B: MeCN:Water 95:5+0.05% Formic acid)) to give the title compound (23 mg)

1. waitThe reaction mixture was left
2. temperatureheated to 120° C. for 2 hr in a microwave
3. customThe cooled reaction mixture
4. concentrationwas concentrated in vacuo
5. customthe residue purified by Mass Directed Preparative HPLC (Supelcosil ABZ+Plus column
6. washeluting with solvents A/B (A: Water+0.1% Formic acid, B