反应详情

温度

150 °C

A mixture of 1-(3-chloroisoquinolin-1-yl)piperidin-4-ylcarbamate (99 mg, 0.27 mmol), 2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-phenol (92 mg, 0.42 mmol), K3PO4 (0.17 g, 0.80 mmol), Pd(OAc)2 (3.9 mg, 17 μmol), Xantphos (6.6 mg, 11 μmol), toluene (1.3 mL), and water (0.1 mL) was sealed in a microwave vessel and heated by microwave irradiation at 150° C. for 10 minutes. The reaction was filtered and purified by reverse phase HPLC (10%-99% CH3CN (0.035% TFA)/H2O (0.05% TFA)) to yield isobutyl 1-(3-(2-hydroxyphenyl)isoquinolin-1-yl)piperidin-4-ylcarbamate. LC/MS: m/z 420.2 (M+H)+ at 3.79 min (10%-99% CH3CN (0.035% TFA)/H2O (0.05% TFA)).

1. customwas sealed in a microwave vessel
2. filtrationThe reaction was filtered
3. custompurified by reverse phase HPLC (10%-99% CH3CN (0.035% TFA)/H2O (0.05% TFA))