反应详情

A microwave vial was charged with HATU (2.5 g, 6.57 mmol), triethylamine (1.48 ml, 10.7 mmol), 3-chloro-4-[(1-methylethyl)oxy]benzoic acid (D3; 1.15 g, 5.34 mmol) and N-hydroxy-5-isoquinolinecarboximidamide (D1; 1 g, 5.34 mmol). The solution was stirred at room temperature for 30 minutes. The reaction vessel was sealed and heated under microwave irradiation at 130° C. for 120 min. After cooling, the reaction mixture was filtered. The isolated grey-brown solid was washed with acetonitrile before being dried in vacuo at 60° C. to give the title compound as a grey solid (738 mg, 37%).

1. customThe reaction vessel was sealed
2. temperatureheated under microwave irradiation at 130° C. for 120 min
3. temperatureAfter cooling
4. filtrationthe reaction mixture was filtered
5. washThe isolated grey-brown solid was washed with acetonitrile
6. custombefore being dried in vacuo at 60° C.