反应 #470450

反应方程式

7-Chloro-3-(3-pyrazol-1-yl-phenyl)-imidazo[1,2-a]pyridine

3-pyridine boronic acid

EtOH

Na2CO3

→

3-(3-pyrazol-1-yl-phenyl)-7-pyridin-3-yl-imidazo[1,2-a]pyridine

溶剂

DME

water

反应条件

后处理

1. 1
   温度the reaction mixture is heated
2. 2
   其他at 120° C.
3. 3
   其他for 15 min
4. 4
   其他At the completion of this time the solvent is removed in vacuo
5. 5
   其他the reaction mixture is purified by flash column chromatography
6. 6
   洗涤eluting with 8:2 DCM/MeOH

实验过程

7-Chloro-3-(3-pyrazol-1-yl-phenyl)-imidazo[1,2-a]pyridine (Intermediate AA) (1 eq, 0.214 mmol, 70 mg) and 3-pyridine boronic acid (1 eq, 0.214 mmol, 26.1 mg) are dissolved in DME (3 ml), EtOH (1 ml) and water (1.5 ml) and Na2CO3 (2 eq, 0.427 mmol, 53.0 mg) is added. Pd(PPh3)4 (0.06 eq, 0.01 mmol, 15 mg) is added and the reaction mixture is heated using microwave radiation at 120° C. for 15 min. At the completion of this time the solvent is removed in vacuo and the reaction mixture is purified by flash column chromatography eluting with 8:2 DCM/MeOH to yield 3-(3-pyrazol-1-yl-phenyl)-7-pyridin-3-yl-imidazo[1,2-a]pyridine as a light brown solid; [M+H]+=338

来源