反应详情

A sealed tube was charged with 123c (200 mg, 0.49 mmol), 3-(acetoxymethyl)-2-(1-oxo-3,4,6,7,8,9-hexahydropyrazino[1,2-a]indol-2(1H)-yl)pyridin-4-ylboronic acid (113i) (188 mg, 0.49 mmol), Pd(dppf)Cl2 (40 mg, 0.049 mmol), K3PO4 (208 mg, 0.98 mmol), NaOAc (133 mg, 0.98 mmol), H2O (3 mL), and MeCN (50 mL). The mixture was heated at 110° for 3 h. The solvent was evaporated in vacuo and the residue was purified by silica gel chromatography eluting with 30:1 DCM/MeOH to 123d (187 mg, 57%). MS: [M+H]+ 667.7.

1. temperatureThe mixture was heated at 110° for 3 h
2. customThe solvent was evaporated in vacuo
3. customthe residue was purified by silica gel chromatography
4. washeluting with 30:1 DCM/MeOH to 123d (187 mg, 57%)