反应详情
EQUATION
反应方程式
REACTANTS
反应物
PRODUCTS
生成物
AUXILIARIES
试剂、催化剂与溶剂
CONDITIONS
反应条件
- 温度
- 120 °C
PROCEDURE
实验过程
Prepared according to procedure N using 4-(6-bromo-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)-7-fluoro-3-methyl-2-(2-methylpyridin-3-yl)-quinoline (41 mg, 0.086 mmol), Pd2dba3 (7.86 mg, 8.59 μmol), morpholine (8.23 μL, 0.094 mmol), sodium tert-butoxide (16.5 mg, 0.172 mmol) and XPhos (8.19 mg, 0.017 mmol) in toluene (1.5 mL) and heating in the microwave for 1 h at 120° C. After purification 4-(3,3-dimethyl-6-(4-morpholinyl)-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)-7-fluoro-3-methyl-2-(2-methyl-3-pyridinyl)quino line was obtained as a yellow film. 1H NMR (400 MHz, chloroform-d) δ ppm 8.66 (1H, dt, J=4.9, 1.7 Hz), 7.78-7.88 (2H, m), 7.67 (1H, d, J=7.6 Hz), 7.57-7.63 (1H, m), 7.30-7.40 (2H, m), 5.84 (1H, d, J=2.0 Hz), 3.70-3.92 (6H, m), 2.93-3.12 (4H, m), 2.42 (3H, s), 2.08 (3H, s), 1.66 (3H, m), 1.59 (3H, s). Mass Spectrum (ESI) m/e=484 (M+1).
WORKUP
后处理
- customPrepared
- customAfter purification 4-(3,3-dimethyl-6-(4-morpholinyl)-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-1-yl)-7-fluoro-3-methyl-2-(2-methyl-3-pyridinyl)quino line
- customwas obtained as a yellow film