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 P using 1-(7-fluoro-3-methyl-2-(pyridin-2-yl)quinolin-4-yl)-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-6-ylboronic acid (92 mg, 0.215 mmol), PdCl2(PPh3)2 (15.12 mg, 0.021 mmol), 2-amine-4-chloropyrimidine (30.6 mg, 0.236 mmol) and sodium carbonate (68.3 mg, 0.644 mmol) in 1,4-dioxane (2.5 mL) and water (0.5 mL) and heating in the microwave for 1 h at 120° C. After purification 4-(1-(7-fluoro-3-methyl-2-(2-pyridinyl)-4-quinolinyl)-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-6-yl)-2-pyrimidinamine was obtained as a yellow solid. 1H NMR (400 MHz, chloroform-d) δ ppm 8.68-8.80 (1H, m), 8.49 (1H, d, J=2.0 Hz), 8.26 (1H, d, J=5.5 Hz), 7.72-7.99 (4H, m), 7.41 (1H, ddd, J=7.0, 5.1, 2.0 Hz), 7.29-7.34 (1H, m), 6.93 (1H, d, J=5.1 Hz), 6.77-6.86 (1H, m), 5.16 (2H, br. s.), 3.77-3.95 (2H, m), 2.27-2.44 (3H, m), 1.61-1.68 (3H, m), 1.51-1.60 (3H, m). Mass Spectrum (ESI) m/e=478 (M+1).
WORKUP
后处理
- customPrepared
- customAfter purification 4-(1-(7-fluoro-3-methyl-2-(2-pyridinyl)-4-quinolinyl)-3,3-dimethyl-2,3-dihydro-1H-pyrrolo[3,2-b]pyridin-6-yl)-2-pyrimidinamine
- customwas obtained as a yellow solid