反应详情

温度

150 °C

To a solution of 1-oxo-N-[3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]-2,3,4,5-tetrahydro-1H-[1,4]diazepino[1,2-a]indole-8-carboxamide in DME:H2O:ethanol (7:3:2 v/v/v, 2.0 mL) is added K3PO4 (34.3 mg, 0.162 mmol) and Pd(dppf)Cl2 CH2Cl2 adduct (11 mg, 0.0135 mmol). The solution is added to a microwave vial containing 3-bromo-1H-pyrazole (29.8 mg, 0.15 mmol). The resulting mixture is heated in a microwave reactor at 150° C. for 30 minutes. The mixture is filtered through Celite (100 mg) washed with ethyl acetate (3×1 mL) and concentrated in vacuo. The residue is purified by mass triggered HPLC to provide the title compound as a (31 mg, 39%).

1. additionThe solution is added to a microwave vial
2. filtrationThe mixture is filtered through Celite (100 mg)
3. washwashed with ethyl acetate (3×1 mL)
4. concentrationconcentrated in vacuo
5. customThe residue is purified by mass